PDGFR

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PDGFR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
S2475 Imatinib Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Cell Commun Signal, 2023, 21(1):342
Phytomedicine, 2023, 117:154918
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
S1026 Imatinib Mesylate Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
bioRxiv, 2024, 10.1101/2024.01.04.574149
Cell Rep Med, 2023, 4(5):101025
Blood Cancer J, 2023, 13(1):42
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
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
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
S2730 Crenolanib Crenolanib is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib helps to induce mitophagy.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
Cell Death Discov, 2023, 9(1):44
Cells, 2023, 12(17)2171
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
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
S1064 Masitinib Masitinib is a novel inhibitor for Kit (c-Kit) and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3.
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
Int J Mol Sci, 2023, 24(11)9708
Molecules, 2023, 28(18)6643
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
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
S1536 CP-673451 CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.
Mil Med Res, 2023, 10(1):13
Pharmaceuticals (Basel), 2023, 17(1)9
Discov Oncol, 2023, 14(1):166
S1470 Orantinib (SU6668) Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
bioRxiv, 2023, 2023.05.11.540170
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.
Microbiol Spectr, 2023, e0510522.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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
S8024 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.
Dev Cell, 2022, 57(12):1466-1481.e6
Front Pharmacol, 2021, 12:804327
Mol Med Rep, 2021, 23(4):1
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
S8553 Avapritinib Avapritinib is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).
Front Immunol, 2023, 14:1078958
Int J Mol Sci, 2023, 24(1)830
Am J Cancer Res, 2023, 13(2):355-378
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
S4736 Trapidil Trapidil (Rocornal, Trapymin, Avantrin, Trapymine) is a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S8757 Ripretinib Ripretinib is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively.
Front Immunol, 2023, 14:1078958
Int J Mol Sci, 2023, 24(1)830
Toxicol Appl Pharmacol, 2023, 466:116490
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
S8015 Agerafenib (CEP-32496) Agerafenib (CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
Mol Pharmacol, 2021, 99(6):435-447
Dis Model Mech, 2020, dmm.047779
Cancer Immunol Res, 2019,
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
S2774 MK-2461 MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. .
Mol Carcinog, 2021, 60(7):481-496
G3 (Bethesda), 2021, 11(10)jkab265
Mol Cell Biochem, 2018, 449(1-2):1-8
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
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
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
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
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
J Cell Sci, 2021, jcs.258685
Molecules, 2020, 8;25(9) pii: E2220
S2895 Tyrphostin 9 Tyrphostin 9 (SF 6847, RG-50872) is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.
Cell Rep, 2022, 38(10):110475
E4449New AG 825 AG-825 (Tyrphostin AG-825) is a potent and selective inhibitor of ErbB2 with IC50 values of 0.15 µM. It also inhibits PDGFR autophosphorylation with IC50 value of 40 µM. It exhibits anti-cancer activity and significantly induces apoptosis in cancer cells.
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.
S4018 Sennoside B Sennoside B, a kind of irritant laxative isolated from rhei rhizome, inhibits PDGF-stimulated cell proliferation.
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.
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.
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.
E0814 Masitinib mesylate Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK.
S8780 AZD3229 AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).
E2548 N-(p-Coumaroyl) Serotonin N-(p-Coumaroyl) Serotonin (p-coumaroylserotonin) is a polyphenol isolated from the seeds of safflower and has antioxidative, anti-atherogenic and anti-inflammatory properties, can inhibits PDGF-induced on phosphorylation of PDGF receptor and Ca2+ release from sarcoplasmic reticulum.
E0050 Seralutinib (GB002) Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively.
E2393 JNJ-10198409 JNJ-10198409, a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor with IC50 of 2 nM, is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent, has good activity against PDGFRβ kinase and PDGFRα kinase with IC50 of 4.2 and 45 nM, respectively.
S9973 Flumatinib (HH-GV-678) Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2  nM, 307.6  nM and 665.5  nM for c-Abl, PDGFRβand c-Kit, respectively.
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
S2475 Imatinib Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Cell Commun Signal, 2023, 21(1):342
Phytomedicine, 2023, 117:154918
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
S1026 Imatinib Mesylate Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
bioRxiv, 2024, 10.1101/2024.01.04.574149
Cell Rep Med, 2023, 4(5):101025
Blood Cancer J, 2023, 13(1):42
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
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
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
S2730 Crenolanib Crenolanib is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib helps to induce mitophagy.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
Cell Death Discov, 2023, 9(1):44
Cells, 2023, 12(17)2171
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
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
S1064 Masitinib Masitinib is a novel inhibitor for Kit (c-Kit) and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3.
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
Int J Mol Sci, 2023, 24(11)9708
Molecules, 2023, 28(18)6643
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
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
S1536 CP-673451 CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.
Mil Med Res, 2023, 10(1):13
Pharmaceuticals (Basel), 2023, 17(1)9
Discov Oncol, 2023, 14(1):166
S1470 Orantinib (SU6668) Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
bioRxiv, 2023, 2023.05.11.540170
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.
Microbiol Spectr, 2023, e0510522.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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
S8024 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.
Dev Cell, 2022, 57(12):1466-1481.e6
Front Pharmacol, 2021, 12:804327
Mol Med Rep, 2021, 23(4):1
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
S8553 Avapritinib Avapritinib is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).
Front Immunol, 2023, 14:1078958
Int J Mol Sci, 2023, 24(1)830
Am J Cancer Res, 2023, 13(2):355-378
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
S8757 Ripretinib Ripretinib is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively.
Front Immunol, 2023, 14:1078958
Int J Mol Sci, 2023, 24(1)830
Toxicol Appl Pharmacol, 2023, 466:116490
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
S8015 Agerafenib (CEP-32496) Agerafenib (CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
Mol Pharmacol, 2021, 99(6):435-447
Dis Model Mech, 2020, dmm.047779
Cancer Immunol Res, 2019,
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
S2774 MK-2461 MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. .
Mol Carcinog, 2021, 60(7):481-496
G3 (Bethesda), 2021, 11(10)jkab265
Mol Cell Biochem, 2018, 449(1-2):1-8
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
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
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
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
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
J Cell Sci, 2021, jcs.258685
Molecules, 2020, 8;25(9) pii: E2220
S2895 Tyrphostin 9 Tyrphostin 9 (SF 6847, RG-50872) is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.
Cell Rep, 2022, 38(10):110475
E4449New AG 825 AG-825 (Tyrphostin AG-825) is a potent and selective inhibitor of ErbB2 with IC50 values of 0.15 µM. It also inhibits PDGFR autophosphorylation with IC50 value of 40 µM. It exhibits anti-cancer activity and significantly induces apoptosis in cancer cells.
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.
S4018 Sennoside B Sennoside B, a kind of irritant laxative isolated from rhei rhizome, inhibits PDGF-stimulated cell proliferation.
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.
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.
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.
E0814 Masitinib mesylate Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK.
S8780 AZD3229 AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).
E2548 N-(p-Coumaroyl) Serotonin N-(p-Coumaroyl) Serotonin (p-coumaroylserotonin) is a polyphenol isolated from the seeds of safflower and has antioxidative, anti-atherogenic and anti-inflammatory properties, can inhibits PDGF-induced on phosphorylation of PDGF receptor and Ca2+ release from sarcoplasmic reticulum.
E0050 Seralutinib (GB002) Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively.
E2393 JNJ-10198409 JNJ-10198409, a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor with IC50 of 2 nM, is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent, has good activity against PDGFRβ kinase and PDGFRα kinase with IC50 of 4.2 and 45 nM, respectively.
S9973 Flumatinib (HH-GV-678) Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2  nM, 307.6  nM and 665.5  nM for c-Abl, PDGFRβand c-Kit, respectively.
S4736 Trapidil Trapidil (Rocornal, Trapymin, Avantrin, Trapymine) is a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00579-z
E4449New AG 825 AG-825 (Tyrphostin AG-825) is a potent and selective inhibitor of ErbB2 with IC50 values of 0.15 µM. It also inhibits PDGFR autophosphorylation with IC50 value of 40 µM. It exhibits anti-cancer activity and significantly induces apoptosis in cancer cells.

PDGFR阻害剤の選択性比較

Tags: PDGFR inhibition | PDGFR mutation | PDGFR cancer | PDGFR pathway | PDGF receptor signaling | PDGFR activation | PDGFR phosphorylation | PDGF receptor activation | PDGFR alpha mutation | PDGFR beta pathway | PDGFR inhibitor review