VEGFR

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VEGFR製品

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S7397 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Genomics, 2024, 116(1):110764
Mol Cell, 2023, 83(5):803-818.e8
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S1040 Sorafenib tosylate Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Cell, 2023, S0092-8674(23)01032-2
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S7781 Sunitinib Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Pharmaceuticals (Basel), 2024, 17(1)77
Heliyon, 2024, 10(3):e24779
Mol Neurodegener, 2023, 18(1):67
S1490 Ponatinib Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Clin Cancer Res, 2023, 29(16):3151-3161
Cell Death Dis, 2023, 14(7):463
S1178 Regorafenib Regorafenibは VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) および Raf-1 に対するマルチターゲット阻害剤であり、cell-free assay における IC50 はそれぞれ 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM です。Regorafenib はオートファジーを誘導します。
Nat Med, 2024, 10.1038/s41591-024-02824-y
NPJ Precis Oncol, 2024, 8(1):52
Signal Transduct Target Ther, 2023, 8(1):65
S1005 Axitinib Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
J Exp Med, 2023, 220(11)e20230011
J Exp Med, 2023, 220(11)e20230011
Theranostics, 2023, 13(11):3744-3760
S1042 Sunitinib malate Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Pharmaceuticals (Basel), 2024, 17(1)108
Cell Cycle, 2024, 1-13.
J Cancer, 2024, 15(5):1429-1441
S1029 Lenalidomide Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.
Clin Immunol, 2024, 260:109915
J Biol Chem, 2024, S0021-9258(24)00128-5
bioRxiv, 2024, :2024.01.22.576669.
S1119 Cabozantinib (XL184) カボザンチニブ (Cabozantinib (XL184, BMS-907351)) は強力な VEGFR2 阻害剤であり、IC50 は 0.035 nM です。また c-Met, Ret, Kit, Flt-1/3/4, Tie2 および AXL に対しても阻害活性があり、cell-free assay における IC50 はそれぞれ 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, 7 nM です。カボザンチニブは大腸がん細胞において AKT/GSK-3β/NF-κB 経路を介して PUMA 依存性アポトーシス (PUMA-dependent apoptosis) を誘発します。
Nat Cancer, 2023, 4(9):1345-1361
Mol Cell, 2023, 83(5):803-818.e8
Biomed Pharmacother, 2023, 164:115002
S1010 Nintedanib Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.
Invest Ophthalmol Vis Sci, 2024, 65(2):30
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
Elife, 2023, 12e79840
S1264 PD173074 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.
Malignancy Spectrum, 2024, 10.1002/msp2.20
JCI Insight, 2023, 8(10)e154729
Oral Oncol, 2023, 146:106562
S1046 Vandetanib Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Nat Cancer, 2023, 4(9):1345-1361
Cell Reports, 2023, 112328
Cell Rep, 2023, 42(4):112328
S1164 Lenvatinib レンバチニブ (Lenvatinib (E7080)) はマルチターゲット阻害剤の一種であり、主に VEGFR2(KDR)/VEGFR3(Flt-4) に対して活性を示し IC50 は 4 nM/5.2 nMである一方、VEGFR1/Flt-1に対しては活性が弱く、cell-free assay において FGFR1, PDGFRα/βよりも VEGFR2/3 に対して 10 倍高い選択性を示します。レンバチニブ (E7080) はまた FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET) も阻害し、強力な抗腫瘍活性を呈します。
Nat Commun, 2024, 15(1):1754
Phytomedicine, 2024, 10.1016/j.phymed.2023.155091
bioRxiv, 2024, 10.1101/2024.01.18.576182
S4001 Cabozantinib malate Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Cancer Sci, 2023, 114(4):1651-1662
PLoS One, 2023, 18(2):e0277306
Adv Sci (Weinh), 2022, e2201478
S1111 Foretinib Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
Int J Mol Sci, 2023, 24(1)757
Biol Open, 2023, 12(8)bio059994
Melanoma Res, 2023, 10.1097/CMR.0000000000000911
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Cancer Sci, 2023, 114(10):4089-4100
Cancer Sci, 2023, 10.1111/cas.15915
Braz J Med Biol Res, 2023, 55:e12206
S1017 Cediranib (AZD2171) Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Cell Oncol (Dordr), 2023, 46(2):391-407
Biochem Pharmacol, 2023, 214:115681
Int J Mol Sci, 2023, 24(9)8037
S1035 Pazopanib HCl Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
iScience, 2023, 26(7):107116
NPJ Breast Cancer, 2022, 8(1):44
J Pers Med, 2022, 12(2)258
S1018 Dovitinib (TKI-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.
Sci Adv, 2023, 9(9):eadd2671
UFTM, 2023,
Cell Rep Med, 2022, 3(1):100492
S1101 Vatalanib (PTK787) 2HCl Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.
J Exp Clin Cancer Res, 2023, 42(1):79
Cancer Med, 2023, 12(15):16416-16430
Cancer Med, 2023, 12(15):16416-16430
S5077 Regorafenib (BAY-734506) Monohydrate Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.
J Clin Med, 2023, 12(23)7267
J Hematol Oncol, 2022, 15(1):109
Life (Basel), 2022, 12(8)1258
S1207 Tivozanib Tivozanib is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3.
Cancer Res, 2023, 83(12):2034-2051
Biochem Pharmacol, 2023, 214:115681
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
A2006 Bevacizumab (anti-VEGF) Bevacizumab (anti-VEGF, Avastin) is a humanized anti-VEGF monoclonal antibody which binds to and neutralizes all human VEGF-A isoforms and bioactive proteolytic fragments, MW:149 KD.
Nat Commun, 2024, 15(1):1359
ESC Heart Fail, 2024, 10.1002/ehf2.14640
Cancer Immunol Res, 2023, 11(11):1493-1507
S8401 Erdafitinib Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.
J Clin Invest, 2024, 134(2)e169241
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
S1003 Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
Cell Death Discov, 2023, 9(1):57
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
S8726 Anlotinib (AL3818) dihydrochloride Anlotinib (AL3818) is a highly potent and selective VEGFR2 inhibitor with IC50 less than 1 nM. It has broad-spectrum antitumor potential in clinical trials. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation.
Cell Rep Med, 2024, 5(2):101416
Braz J Med Biol Res, 2024, 57:e13152
Front Pharmacol, 2023, 14:1189245
S7765 Dovitinib (TKI258) Lactate monohydrate Dovitinib (TKI258) Lactate monohydrate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
Mol Cell, 2021, S1097-2765(21)00507-4
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancer Res, 2021, canres.1780.2020
S5240 Lenvatinib Mesylate Lenvatinib Mesylate is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.
Nat Commun, 2024, 15(1):1754
J Hepatocell Carcinoma, 2023, 10:697-712
Discov Oncol, 2023, 14(1):26
S2161 RAF265 (CHIR-265) RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00312-9
iScience, 2022, 25(10):105182
Cancers (Basel), 2022, 14(6)1575
S2842 SAR131675 SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.
Cell Rep, 2023, 42(5):112489
J Orthop Translat, 2023, 38:65-75
Cell Signal, 2023, 111:110856
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Sci Rep, 2024, 14(1):879
Adv Sci (Weinh), 2023, 10(23):e2300898
J Thorac Oncol, 2023, S1556-0864(23)00802-X
S2221 Apatinib (YN968D1) mesylate Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S4947 Regorafenib Hydrochloride Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
Cancers (Basel), 2023, 15(18)4477
Cancers (Basel), 2023, 15(18)4477
J Clin Med, 2023, 12(23)7267
S1363 Ki8751 Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
Drug Des Devel Ther, 2023, 17:1567-1582
Transl Oncol, 2022, 25:101516
Front Oncol, 2021, 11:650052
S2896 ZM 323881 HCl ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.
Stem Cells Transl Med, 2023, szad049
Stem Cells Transl Med, 2023, 12(10):676-688
iScience, 2023, 26(9):107548
S2845 Semaxanib (SU5416) Semaxanib (SU5416, semaxinib) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3.
Front Immunol, 2022, 13:1035667
Front Neurol, 2021, 12:808568
Pulm Circ, 2021, 11(4):20458940211046156
S7057 LY2874455 LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
S5234 Nintedanib Ethanesulfonate Salt Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively.
Am J Cancer Res, 2023, 13(2):355-378
Theranostics, 2022, 12(2):747-766
EMBO Mol Med, 2022, 14(3):e15295
S7667 SU5402 SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
Regen Ther, 2024, 25:229-237
Dis Model Mech, 2023, 16(7)dmm050066
Immunity, 2022, S1074-7613(22)00291-6
S1486 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.
Cell Rep Med, 2022, 3(1):100492
Genome Med, 2020, 18;12(1):17
Oncotarget, 2019, 10(68):7185-7197
S5242 Cediranib Maleate Cediranib Maleate (AZD2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.
J Exp Clin Cancer Res, 2024, 43(1):56
Cell Oncol (Dordr), 2022, 45(4):601-619
Mol Cancer Ther, 2022, 21(6):1030-1043
S1032 Motesanib Diphosphate (AMG-706) Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.
Front Cell Dev Biol, 2022, 10:836179
J Pharm Sci, 2022, 111(8):2180-2190
Drug Metab Dispos, 2021, 49(1):53-61
S1361 MGCD-265 analog MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
Protein Cell, 2019, 10(3):161-177
S1084 Brivanib (BMS-540215) Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.
Stem Cells Transl Med, 2023, szad049
Stem Cells Transl Med, 2023, 12(10):676-688
iScience, 2023, 26(9):107548
S2897 ZM 306416 ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.
J Pharmacol Sci, 2023, 151(4):177-186
J Dent Sci, 2022, 17(4):1471-1479
Life Sci, 2021, 276:119401
S5793 Motesanib (AMG-706) Motesanib (AMG-706) is an orally bioavailable receptor tyrosine kinase inhibitor with IC50 values of 2 nM, 3 nM, 6 nM, 8 nM, 84 nM, 59 nM for VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR and Ret, respectively.
Signal Transduct Target Ther, 2022, 7(1):147
Front Cell Dev Biol, 2022, 10:836179
J Pharm Sci, 2022, 111(8):2180-2190
S1181 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1171 CYC116 CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
Sci Rep, 2024, 14(1):4303
Cell Chem Biol, 2023, 30(8):987-998.e24
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
S2859 Golvatinib (E7050) Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.
Int J Mol Sci, 2023, 24(11)9606
Int J Mol Sci, 2022, 23(23)14884
Cancer Sci, 2020, 111(10):3813-3823
S4686 Vitamin E Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.
medRxiv, 2023, 10.1101/2023.12.01.23299102
Bone Res, 2022, 10(1):26
J Exp Clin Cancer Res, 2022, 41(1):86
S1220 OSI-930 OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.
Cell Rep, 2019, 28(9):2331-2344
Nat Biomed Eng, 2018, 2(8):578-588
Mol Syst Biol, 2015, 11(1):789
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
PLoS One, 2016, 11(10):e0164895
S1557 KRN 633 KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.
Aust Dent J, 2020, 10.1111/adj.12752
J Med Invest, 2017, 64(3.4):262-265
Oncotarget, 2016, 7(5):5985-99
S2231 Telatinib Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.
Sci Adv, 2022, 8(6):eabg9455
Leiden University Scholarly Publications, 2020, N/A
Cell Stem Cell, 2019, 24(4):654-669
S5667 Fruquintinib Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases.
Cancer Commun (Lond), 2023, 10.1002/cac2.12411
Dev Cell, 2022, 57(12):1466-1481.e6
CellPress, 2021, None
S8573 Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
JCI Insight, 2022, e148717
Cancers (Basel), 2021, 13(21)5474
Cancers (Basel), 2020, 12(1)
S7258 SKLB1002 SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
Dis Model Mech, 2023, 16(5)dmm049571
Exp Cell Res, 2018, 364(2):208-216
BMC Cancer, 2017, 17(1):593
S7003 AZD2932 AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
Cancer Res, 2020, canres.1992.2020
Molecules, 2020, 8;25(9) pii: E2220
Development, 2016, 143(23):4394-4404
S2366 Taxifolin (Dihydroquercetin) Taxifolin, type I inhibitor for VEGFR-2 kinase, is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.
Sci Rep, 2020, 10(1):17311
J Med Virol, 2019, 91(8):1440-1447
Cytotechnology, 2016, 68(4):1633-40
S1138 Brivanib Alaninate (BMS-582664) Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.
Int J Oncol, 2014, 44(3):959-69
Assay Drug Dev Technol, 2014, 12(9-10):514-26
S8189 BAW2881 (NVP-BAW2881) BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations.
JCI Insight, 2021, 143285
J Cell Biochem, 2019, 120(4):5583-5596
S0504 SU14813 SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity.
Cancer Cell, 2022, S1535-6108(22)00312-9
Adv Sci (Weinh), 2021, e2101848
S6535 SU1498 SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells.
Cell Metab, 2020, 5;31(5):892-908 e11
Biol Open, 2018,
S8721 PDGFR inhibitor 1 PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth.
Elife, 2023, 12e79840
Elife, 2023, 12e79840
Oncogene, 2022, 41(20):2860-2872
S0278 SU5614 SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis.
Adv Sci (Weinh), 2021, e2101848
Front Cell Dev Biol, 2021, 9:797047
S6526 SKLB 610 SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR.
Biomed Pharmacother, 2022, 149:112922
Int J Mol Sci, 2022, 23(14)7853
S6412 Altiratinib Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S6514 SU5408 SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM.
Transl Oncol, 2022, 25:101516
J Dent Sci, 2022, 17(4):1471-1479
S2201 BMS-794833 BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.
Cancer Res, 2021, canres.1428.2021
S0290 SU5204 SU5204, an analogue of SU5025, is a pharmacological inhibitor of VEGFR2.
Front Pharmacol, 2021, 12:804327
A2003 Ramucirumab (anti-VEGFR2) Ramucirumab is a monoclonal antibody of the IgG1 class that binds to VEGF-R2 and prevents its activation. The IC50 value for blocking KDR binding to VEGF is 0.8 nM for ramucirumab, MW : 143.6 KD.
Int J Mol Sci, 2024,
JTO Clin Res Rep, 2023, 4(6):100525
S0487 Sulfatinib Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.
Front Oncol, 2023, 13:1158857
S2018 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
S6520 WHI-P180 WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively.
S6543 ZD-4190 ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
S7688 Ki20227 Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.
S5272 Toceranib phosphate Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively.
S8188 BFH772 BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
S0291 SU5208 SU5208(3-[(Thien-2-yl)methylene]-2-indolinone) is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR2).
A2126New Anti-mouse VEGFR-2-InVivo Anti-mouse VEGFR-2-InVivo (Clone: DC101) monoclonal antibody reacts with mouse VEGFR-2 (vascular endothelial growth factor receptor 2) also known as CD309, KDR, and Flk-1 and inhibit VEGFR-2 signaling in vivo. VEGFR-2 plays a key role in vascular development and permeability.
E2397 hVEGF-IN-1 hVEGF-IN-1, a quinazoline derivative, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) with a Kd of 0.928 μM, therefore destabilizes the G-quadruplex structure, , also hinders tumor cells migration and represses tumor growth by decreasing VEGF-A protein expression.
S8882 ODM-203 ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.
S0763 Tyrphostin AG1433 Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively.
S0765 MAZ51 MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
E0499 4SC-203 4SC-203 (SC71710) is a multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs).
S2431 TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
E2656 R1530 R1530 is a highly potent, orally bioavailable, dual-acting mitosis/angiogenesis inhibitor for the treatment of solid tumors, which can inhibit vascular endothelial growth factor receptor 2 (VEGFR2) and fibroblast growth factor receptors 1 (FGFR1) with IC50s of 10 nM and 28 nM, respectively.
S9621 Donafenib (Sorafenib D3) Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively.
E1078 Emvododstat (PTC299) Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM.
S2211 AG-13958 AG-13958 (AG-013958), a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD).
S5607 4,4'-Bis(4-aminophenoxy)biphenyl 4,4'-Bis(4-aminophenoxy)biphenyl is a monomer for polyimide production.
S7647 Lucitanib (E3810) hydrochloride Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
E0616 Chiauranib Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
S6870 Ningetinib Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity.
S6843 Vorolanib Vorolanib (X-82,CM082) is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities.
S6764 Pamufetinib (TAS-115) Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively.
S6939 Nastorazepide Nastorazepide (Z-360), a cholecystokinin-2/gastrin receptor (CCK2/gastrin receptor) antagonist, combines with gemcitabine prolonged survival and reduces gemcitabine-induced vascular endothelial growth factor (VEGF) expression in a pancreatic carcinoma orthotopic xenograft mouse.
S0377 CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) 是一种耐受性良好的、口服有效的、高选择性的 VEGFR-2 抑制剂,IC50值为40 nM。CS-2660(JNJ-38158471)还抑制紧密相关的酪氨酸激酶,如 RET (c-RET)Kit (c-Kit),IC50为180 nM和500 nM,但无明显活性 (>1 microM) 针对VEGFR-1和VEGFR-3。
S9402 (20R)-Protopanaxadiol (20R)-Protopanaxadiol, isolated from the roots of Panax ginseng, has protective effect on myocardial ischemia.
E0207 Chebulinic acid Chebulinic acid, a phenolic compound isolated from Terminalia chebula fruit, is a novel Influenza viral neuraminidase inhibitor. Chebulinic acid is a antiangiogenic agent through inhibiting the actions of VEGF. Chebulinic acid shows antitumour activity.
S6808 SU5205 SU5205 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 9.6 µM.
S6809 SU5214 SU5214 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).
E0142 XL092 XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
A2126New Anti-mouse VEGFR-2-InVivo Anti-mouse VEGFR-2-InVivo (Clone: DC101) monoclonal antibody reacts with mouse VEGFR-2 (vascular endothelial growth factor receptor 2) also known as CD309, KDR, and Flk-1 and inhibit VEGFR-2 signaling in vivo. VEGFR-2 plays a key role in vascular development and permeability.
S7397 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Genomics, 2024, 116(1):110764
Mol Cell, 2023, 83(5):803-818.e8
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S1040 Sorafenib tosylate Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Cell, 2023, S0092-8674(23)01032-2
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S7781 Sunitinib Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Pharmaceuticals (Basel), 2024, 17(1)77
Heliyon, 2024, 10(3):e24779
Mol Neurodegener, 2023, 18(1):67
S1490 Ponatinib Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Clin Cancer Res, 2023, 29(16):3151-3161
Cell Death Dis, 2023, 14(7):463
S1178 Regorafenib Regorafenibは VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) および Raf-1 に対するマルチターゲット阻害剤であり、cell-free assay における IC50 はそれぞれ 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM です。Regorafenib はオートファジーを誘導します。
Nat Med, 2024, 10.1038/s41591-024-02824-y
NPJ Precis Oncol, 2024, 8(1):52
Signal Transduct Target Ther, 2023, 8(1):65
S1005 Axitinib Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
J Exp Med, 2023, 220(11)e20230011
J Exp Med, 2023, 220(11)e20230011
Theranostics, 2023, 13(11):3744-3760
S1042 Sunitinib malate Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Pharmaceuticals (Basel), 2024, 17(1)108
Cell Cycle, 2024, 1-13.
J Cancer, 2024, 15(5):1429-1441
S1029 Lenalidomide Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.
Clin Immunol, 2024, 260:109915
J Biol Chem, 2024, S0021-9258(24)00128-5
bioRxiv, 2024, :2024.01.22.576669.
S1119 Cabozantinib (XL184) カボザンチニブ (Cabozantinib (XL184, BMS-907351)) は強力な VEGFR2 阻害剤であり、IC50 は 0.035 nM です。また c-Met, Ret, Kit, Flt-1/3/4, Tie2 および AXL に対しても阻害活性があり、cell-free assay における IC50 はそれぞれ 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, 7 nM です。カボザンチニブは大腸がん細胞において AKT/GSK-3β/NF-κB 経路を介して PUMA 依存性アポトーシス (PUMA-dependent apoptosis) を誘発します。
Nat Cancer, 2023, 4(9):1345-1361
Mol Cell, 2023, 83(5):803-818.e8
Biomed Pharmacother, 2023, 164:115002
S1010 Nintedanib Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.
Invest Ophthalmol Vis Sci, 2024, 65(2):30
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
Elife, 2023, 12e79840
S1264 PD173074 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.
Malignancy Spectrum, 2024, 10.1002/msp2.20
JCI Insight, 2023, 8(10)e154729
Oral Oncol, 2023, 146:106562
S1046 Vandetanib Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Nat Cancer, 2023, 4(9):1345-1361
Cell Reports, 2023, 112328
Cell Rep, 2023, 42(4):112328
S1164 Lenvatinib レンバチニブ (Lenvatinib (E7080)) はマルチターゲット阻害剤の一種であり、主に VEGFR2(KDR)/VEGFR3(Flt-4) に対して活性を示し IC50 は 4 nM/5.2 nMである一方、VEGFR1/Flt-1に対しては活性が弱く、cell-free assay において FGFR1, PDGFRα/βよりも VEGFR2/3 に対して 10 倍高い選択性を示します。レンバチニブ (E7080) はまた FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET) も阻害し、強力な抗腫瘍活性を呈します。
Nat Commun, 2024, 15(1):1754
Phytomedicine, 2024, 10.1016/j.phymed.2023.155091
bioRxiv, 2024, 10.1101/2024.01.18.576182
S4001 Cabozantinib malate Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Cancer Sci, 2023, 114(4):1651-1662
PLoS One, 2023, 18(2):e0277306
Adv Sci (Weinh), 2022, e2201478
S1111 Foretinib Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
Int J Mol Sci, 2023, 24(1)757
Biol Open, 2023, 12(8)bio059994
Melanoma Res, 2023, 10.1097/CMR.0000000000000911
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Cancer Sci, 2023, 114(10):4089-4100
Cancer Sci, 2023, 10.1111/cas.15915
Braz J Med Biol Res, 2023, 55:e12206
S1017 Cediranib (AZD2171) Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Cell Oncol (Dordr), 2023, 46(2):391-407
Biochem Pharmacol, 2023, 214:115681
Int J Mol Sci, 2023, 24(9)8037
S1035 Pazopanib HCl Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
iScience, 2023, 26(7):107116
NPJ Breast Cancer, 2022, 8(1):44
J Pers Med, 2022, 12(2)258
S1018 Dovitinib (TKI-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.
Sci Adv, 2023, 9(9):eadd2671
UFTM, 2023,
Cell Rep Med, 2022, 3(1):100492
S1101 Vatalanib (PTK787) 2HCl Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.
J Exp Clin Cancer Res, 2023, 42(1):79
Cancer Med, 2023, 12(15):16416-16430
Cancer Med, 2023, 12(15):16416-16430
S5077 Regorafenib (BAY-734506) Monohydrate Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.
J Clin Med, 2023, 12(23)7267
J Hematol Oncol, 2022, 15(1):109
Life (Basel), 2022, 12(8)1258
S1207 Tivozanib Tivozanib is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3.
Cancer Res, 2023, 83(12):2034-2051
Biochem Pharmacol, 2023, 214:115681
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
S8401 Erdafitinib Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.
J Clin Invest, 2024, 134(2)e169241
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
S1003 Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
Cell Death Discov, 2023, 9(1):57
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
S8726 Anlotinib (AL3818) dihydrochloride Anlotinib (AL3818) is a highly potent and selective VEGFR2 inhibitor with IC50 less than 1 nM. It has broad-spectrum antitumor potential in clinical trials. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation.
Cell Rep Med, 2024, 5(2):101416
Braz J Med Biol Res, 2024, 57:e13152
Front Pharmacol, 2023, 14:1189245
S7765 Dovitinib (TKI258) Lactate monohydrate Dovitinib (TKI258) Lactate monohydrate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
Mol Cell, 2021, S1097-2765(21)00507-4
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancer Res, 2021, canres.1780.2020
S5240 Lenvatinib Mesylate Lenvatinib Mesylate is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.
Nat Commun, 2024, 15(1):1754
J Hepatocell Carcinoma, 2023, 10:697-712
Discov Oncol, 2023, 14(1):26
S2161 RAF265 (CHIR-265) RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00312-9
iScience, 2022, 25(10):105182
Cancers (Basel), 2022, 14(6)1575
S2842 SAR131675 SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.
Cell Rep, 2023, 42(5):112489
J Orthop Translat, 2023, 38:65-75
Cell Signal, 2023, 111:110856
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Sci Rep, 2024, 14(1):879
Adv Sci (Weinh), 2023, 10(23):e2300898
J Thorac Oncol, 2023, S1556-0864(23)00802-X
S2221 Apatinib (YN968D1) mesylate Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S4947 Regorafenib Hydrochloride Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
Cancers (Basel), 2023, 15(18)4477
Cancers (Basel), 2023, 15(18)4477
J Clin Med, 2023, 12(23)7267
S1363 Ki8751 Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
Drug Des Devel Ther, 2023, 17:1567-1582
Transl Oncol, 2022, 25:101516
Front Oncol, 2021, 11:650052
S2896 ZM 323881 HCl ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.
Stem Cells Transl Med, 2023, szad049
Stem Cells Transl Med, 2023, 12(10):676-688
iScience, 2023, 26(9):107548
S2845 Semaxanib (SU5416) Semaxanib (SU5416, semaxinib) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3.
Front Immunol, 2022, 13:1035667
Front Neurol, 2021, 12:808568
Pulm Circ, 2021, 11(4):20458940211046156
S7057 LY2874455 LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
S5234 Nintedanib Ethanesulfonate Salt Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively.
Am J Cancer Res, 2023, 13(2):355-378
Theranostics, 2022, 12(2):747-766
EMBO Mol Med, 2022, 14(3):e15295
S7667 SU5402 SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
Regen Ther, 2024, 25:229-237
Dis Model Mech, 2023, 16(7)dmm050066
Immunity, 2022, S1074-7613(22)00291-6
S1486 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.
Cell Rep Med, 2022, 3(1):100492
Genome Med, 2020, 18;12(1):17
Oncotarget, 2019, 10(68):7185-7197
S5242 Cediranib Maleate Cediranib Maleate (AZD2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.
J Exp Clin Cancer Res, 2024, 43(1):56
Cell Oncol (Dordr), 2022, 45(4):601-619
Mol Cancer Ther, 2022, 21(6):1030-1043
S1032 Motesanib Diphosphate (AMG-706) Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.
Front Cell Dev Biol, 2022, 10:836179
J Pharm Sci, 2022, 111(8):2180-2190
Drug Metab Dispos, 2021, 49(1):53-61
S1361 MGCD-265 analog MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
Protein Cell, 2019, 10(3):161-177
S1084 Brivanib (BMS-540215) Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.
Stem Cells Transl Med, 2023, szad049
Stem Cells Transl Med, 2023, 12(10):676-688
iScience, 2023, 26(9):107548
S2897 ZM 306416 ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.
J Pharmacol Sci, 2023, 151(4):177-186
J Dent Sci, 2022, 17(4):1471-1479
Life Sci, 2021, 276:119401
S5793 Motesanib (AMG-706) Motesanib (AMG-706) is an orally bioavailable receptor tyrosine kinase inhibitor with IC50 values of 2 nM, 3 nM, 6 nM, 8 nM, 84 nM, 59 nM for VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR and Ret, respectively.
Signal Transduct Target Ther, 2022, 7(1):147
Front Cell Dev Biol, 2022, 10:836179
J Pharm Sci, 2022, 111(8):2180-2190
S1181 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1171 CYC116 CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
Sci Rep, 2024, 14(1):4303
Cell Chem Biol, 2023, 30(8):987-998.e24
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
S2859 Golvatinib (E7050) Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.
Int J Mol Sci, 2023, 24(11)9606
Int J Mol Sci, 2022, 23(23)14884
Cancer Sci, 2020, 111(10):3813-3823
S4686 Vitamin E Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.
medRxiv, 2023, 10.1101/2023.12.01.23299102
Bone Res, 2022, 10(1):26
J Exp Clin Cancer Res, 2022, 41(1):86
S1220 OSI-930 OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.
Cell Rep, 2019, 28(9):2331-2344
Nat Biomed Eng, 2018, 2(8):578-588
Mol Syst Biol, 2015, 11(1):789
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
PLoS One, 2016, 11(10):e0164895
S1557 KRN 633 KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.
Aust Dent J, 2020, 10.1111/adj.12752
J Med Invest, 2017, 64(3.4):262-265
Oncotarget, 2016, 7(5):5985-99
S2231 Telatinib Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.
Sci Adv, 2022, 8(6):eabg9455
Leiden University Scholarly Publications, 2020, N/A
Cell Stem Cell, 2019, 24(4):654-669
S5667 Fruquintinib Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases.
Cancer Commun (Lond), 2023, 10.1002/cac2.12411
Dev Cell, 2022, 57(12):1466-1481.e6
CellPress, 2021, None
S8573 Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
JCI Insight, 2022, e148717
Cancers (Basel), 2021, 13(21)5474
Cancers (Basel), 2020, 12(1)
S7258 SKLB1002 SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
Dis Model Mech, 2023, 16(5)dmm049571
Exp Cell Res, 2018, 364(2):208-216
BMC Cancer, 2017, 17(1):593
S7003 AZD2932 AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
Cancer Res, 2020, canres.1992.2020
Molecules, 2020, 8;25(9) pii: E2220
Development, 2016, 143(23):4394-4404
S2366 Taxifolin (Dihydroquercetin) Taxifolin, type I inhibitor for VEGFR-2 kinase, is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.
Sci Rep, 2020, 10(1):17311
J Med Virol, 2019, 91(8):1440-1447
Cytotechnology, 2016, 68(4):1633-40
S1138 Brivanib Alaninate (BMS-582664) Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.
Int J Oncol, 2014, 44(3):959-69
Assay Drug Dev Technol, 2014, 12(9-10):514-26
S8189 BAW2881 (NVP-BAW2881) BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations.
JCI Insight, 2021, 143285
J Cell Biochem, 2019, 120(4):5583-5596
S0504 SU14813 SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity.
Cancer Cell, 2022, S1535-6108(22)00312-9
Adv Sci (Weinh), 2021, e2101848
S6535 SU1498 SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells.
Cell Metab, 2020, 5;31(5):892-908 e11
Biol Open, 2018,
S8721 PDGFR inhibitor 1 PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth.
Elife, 2023, 12e79840
Elife, 2023, 12e79840
Oncogene, 2022, 41(20):2860-2872
S0278 SU5614 SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis.
Adv Sci (Weinh), 2021, e2101848
Front Cell Dev Biol, 2021, 9:797047
S6526 SKLB 610 SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR.
Biomed Pharmacother, 2022, 149:112922
Int J Mol Sci, 2022, 23(14)7853
S6412 Altiratinib Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S6514 SU5408 SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM.
Transl Oncol, 2022, 25:101516
J Dent Sci, 2022, 17(4):1471-1479
S2201 BMS-794833 BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.
Cancer Res, 2021, canres.1428.2021
S0290 SU5204 SU5204, an analogue of SU5025, is a pharmacological inhibitor of VEGFR2.
Front Pharmacol, 2021, 12:804327
S0487 Sulfatinib Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.
Front Oncol, 2023, 13:1158857
S2018 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
S6520 WHI-P180 WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively.
S6543 ZD-4190 ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
S7688 Ki20227 Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.
S5272 Toceranib phosphate Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively.
S8188 BFH772 BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
S0291 SU5208 SU5208(3-[(Thien-2-yl)methylene]-2-indolinone) is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR2).
E2397 hVEGF-IN-1 hVEGF-IN-1, a quinazoline derivative, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) with a Kd of 0.928 μM, therefore destabilizes the G-quadruplex structure, , also hinders tumor cells migration and represses tumor growth by decreasing VEGF-A protein expression.
S8882 ODM-203 ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.
S0763 Tyrphostin AG1433 Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively.
S0765 MAZ51 MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
E0499 4SC-203 4SC-203 (SC71710) is a multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs).
E2656 R1530 R1530 is a highly potent, orally bioavailable, dual-acting mitosis/angiogenesis inhibitor for the treatment of solid tumors, which can inhibit vascular endothelial growth factor receptor 2 (VEGFR2) and fibroblast growth factor receptors 1 (FGFR1) with IC50s of 10 nM and 28 nM, respectively.
S9621 Donafenib (Sorafenib D3) Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively.
E1078 Emvododstat (PTC299) Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM.
S2211 AG-13958 AG-13958 (AG-013958), a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD).
S5607 4,4'-Bis(4-aminophenoxy)biphenyl 4,4'-Bis(4-aminophenoxy)biphenyl is a monomer for polyimide production.
S7647 Lucitanib (E3810) hydrochloride Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
E0616 Chiauranib Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
S6870 Ningetinib Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity.
S6843 Vorolanib Vorolanib (X-82,CM082) is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities.
S6764 Pamufetinib (TAS-115) Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively.
S6939 Nastorazepide Nastorazepide (Z-360), a cholecystokinin-2/gastrin receptor (CCK2/gastrin receptor) antagonist, combines with gemcitabine prolonged survival and reduces gemcitabine-induced vascular endothelial growth factor (VEGF) expression in a pancreatic carcinoma orthotopic xenograft mouse.
S0377 CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) 是一种耐受性良好的、口服有效的、高选择性的 VEGFR-2 抑制剂,IC50值为40 nM。CS-2660(JNJ-38158471)还抑制紧密相关的酪氨酸激酶,如 RET (c-RET)Kit (c-Kit),IC50为180 nM和500 nM,但无明显活性 (>1 microM) 针对VEGFR-1和VEGFR-3。
E0207 Chebulinic acid Chebulinic acid, a phenolic compound isolated from Terminalia chebula fruit, is a novel Influenza viral neuraminidase inhibitor. Chebulinic acid is a antiangiogenic agent through inhibiting the actions of VEGF. Chebulinic acid shows antitumour activity.
S6808 SU5205 SU5205 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 9.6 µM.
S6809 SU5214 SU5214 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).
E0142 XL092 XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
A2006 Bevacizumab (anti-VEGF) Bevacizumab (anti-VEGF, Avastin) is a humanized anti-VEGF monoclonal antibody which binds to and neutralizes all human VEGF-A isoforms and bioactive proteolytic fragments, MW:149 KD.
Nat Commun, 2024, 15(1):1359
ESC Heart Fail, 2024, 10.1002/ehf2.14640
Cancer Immunol Res, 2023, 11(11):1493-1507
A2003 Ramucirumab (anti-VEGFR2) Ramucirumab is a monoclonal antibody of the IgG1 class that binds to VEGF-R2 and prevents its activation. The IC50 value for blocking KDR binding to VEGF is 0.8 nM for ramucirumab, MW : 143.6 KD.
Int J Mol Sci, 2024,
JTO Clin Res Rep, 2023, 4(6):100525
S2431 TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
A2126New Anti-mouse VEGFR-2-InVivo Anti-mouse VEGFR-2-InVivo (Clone: DC101) monoclonal antibody reacts with mouse VEGFR-2 (vascular endothelial growth factor receptor 2) also known as CD309, KDR, and Flk-1 and inhibit VEGFR-2 signaling in vivo. VEGFR-2 plays a key role in vascular development and permeability.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).

VEGFR阻害剤の選択性比較

Tags: VEGFR inhibition | VEGFR cancer | VEGFR2 cancer | VEGFR pathway | VEGFR phosphorylation | VEGFR2 phosphorylation | VEGFR signaling pathway | VEGFR assay | VEGFR inhibitor drug | VEGFR inhibitor review