FGFR

亜型選択性的な製品

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FGFRシグナル伝達経路

FGFR製品

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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
S2183 Infigratinib (BGJ398) Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
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
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
S2801 AZD4547 AZD4547 (ABSK 091) is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3.
Cell Death Dis, 2024, 15(1):64
Acta Pharmaceutica Sinica B, 2024, 10.1016/j.apsb.2024.01.013
Cancer Discov, 2023, 13(9):1998-2011
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
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
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
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
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Sci Rep, 2024, 14(1):4303
Proc Natl Acad Sci U S A, 2023, 120(34):e2304611120
Cell Chem Biol, 2023, 30(8):987-998.e24
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
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
S7819 BLU9931 BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.
J Exp Clin Cancer Res, 2023, 42(1):96
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
Medicina (Kaunas), 2023, 10.3390/medicina59091635
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
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
S0088 Pemigatinib Pemigatinib is an orally active and selective inhibitor of FGFR with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
S7665 Zoligratinib (Debio-1347) Zoligratinib (Debio-1347, CH5183284, FF284) is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
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
S8848 Futibatinib (TAS-120) Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
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
S8493 PD-166866 PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1.
J Clin Invest, 2022, e157399
Dis Model Mech, 2022, 15(8)dmm049436
Syst Biol Reprod Med, 2022, 1-15
S7167 SSR128129E SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
BMC Biol, 2021, 19(1):173
Front Oncol, 2021, 11:609918
Sci Rep, 2021, 11(1):6104
S8675 H3B-6527 H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively).
iScience, 2024, 27(2):108841
J Exp Clin Cancer Res, 2023, 42(1):96
Front Cardiovasc Med, 2023, 10:990422
S8503 Fisogatinib (BLU-554) Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM.
Adv Sci (Weinh), 2023, 10(24):e2302613
Acta Neuropathol Commun, 2022, 10(1):65
Biochem Biophys Res Commun, 2022, 595:22-27
S8609 Derazantinib Derazantinib is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
S7714 FIIN-2 FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.
J Biol Chem, 2023, 299(6):104776
Cell Death Dis, 2022, 13(8):750
Front Oncol, 2020, 10;10:331
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
S2300 Ferulic Acid Ferulic Acid (Fumalic) is a hydroxycinnamic acid and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong. Ferulic acid is a novel fibroblast growth factor receptor (FGFR) inhibitor with IC50s of 3.78 μM and 12.5 μM for FGFR1 and FGFR2, respectively.
Pharm Biol, 2022, 60(1):2286-2294
J Med Virol, 2019, 91(8):1440-1447
Biomed Pharmacother, 2019, 120:109482
S6539 ASP5878 ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.
J Biol Chem, 2021, S0021-9258(21)00950-9
bioRxiv, 2020, 10.1101/2020.05.20.107326
bioRxiv, 2020, 10.1101/2020.05.20.107326
S9031 Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
Chem Biol Interact, 2023, 382:110602
Oncotarget, 2021, 12(6):549-561
Cancer Lett, 2020, 469:277-286
S8548 Roblitinib (FGF401) FGF401 is an FGFR4-selective inhibitor with an IC50 of 1.9 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays.
J Exp Clin Cancer Res, 2023, 42(1):96
Br J Cancer, 2022, 10.1038/s41416-022-01973-6
Front Oncol, 2022, 12:936952
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
S8754 Alofanib (RPT835) Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
Cell Death Dis, 2022, 13(8):724
JCI Insight, 2022, e157874
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
S7940 NSC12 NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.
Biomed Pharmacother, 2018, 107:359-367
S8404 S49076 S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.
Mol Brain, 2020, 4;13(1):66
S8578 PRN1371 PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.
Nat Commun, 2021, 12(1):6572
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
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.
E4474New Infigratinib Phosphate Infigratinib Phosphate (NVP-BGJ398 phosphate) is the phosphate salt form of infigratinib, an orally bioavailable pan-inhibitor of human fibroblast growth factor receptors (FGFRs) with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively. It also has potential antiangiogenic, antineoplastic and antitumor activities.
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.
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.
S8192 SUN11602 SUN11602 is a small synthetic compound that mimics the neuroprotective activities of bFGF and activates key molecules in the FGF receptor-1-mitogen-activated protein kinase/extracellular signal-regulated kinase-1/2 kinase (FGFR-1-MEK/ERK) signaling pathway.
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.
S8965 BO-264 BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.
E1431New Lirafugratinib Lirafugratinib (RLY-4008) is an orally active and selective inhibitor of FGFR2.
S7715 FIIN-3 FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, 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).
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
S2183 Infigratinib (BGJ398) Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
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
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
S2801 AZD4547 AZD4547 (ABSK 091) is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3.
Cell Death Dis, 2024, 15(1):64
Acta Pharmaceutica Sinica B, 2024, 10.1016/j.apsb.2024.01.013
Cancer Discov, 2023, 13(9):1998-2011
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
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
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
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
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Sci Rep, 2024, 14(1):4303
Proc Natl Acad Sci U S A, 2023, 120(34):e2304611120
Cell Chem Biol, 2023, 30(8):987-998.e24
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
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
S7819 BLU9931 BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.
J Exp Clin Cancer Res, 2023, 42(1):96
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
Medicina (Kaunas), 2023, 10.3390/medicina59091635
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
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
S0088 Pemigatinib Pemigatinib is an orally active and selective inhibitor of FGFR with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
S7665 Zoligratinib (Debio-1347) Zoligratinib (Debio-1347, CH5183284, FF284) is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
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
S8848 Futibatinib (TAS-120) Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
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
S8493 PD-166866 PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1.
J Clin Invest, 2022, e157399
Dis Model Mech, 2022, 15(8)dmm049436
Syst Biol Reprod Med, 2022, 1-15
S7167 SSR128129E SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
BMC Biol, 2021, 19(1):173
Front Oncol, 2021, 11:609918
Sci Rep, 2021, 11(1):6104
S8675 H3B-6527 H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively).
iScience, 2024, 27(2):108841
J Exp Clin Cancer Res, 2023, 42(1):96
Front Cardiovasc Med, 2023, 10:990422
S8503 Fisogatinib (BLU-554) Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM.
Adv Sci (Weinh), 2023, 10(24):e2302613
Acta Neuropathol Commun, 2022, 10(1):65
Biochem Biophys Res Commun, 2022, 595:22-27
S8609 Derazantinib Derazantinib is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
Cancer Discov, 2023, 13(9):1998-2011
S7714 FIIN-2 FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.
J Biol Chem, 2023, 299(6):104776
Cell Death Dis, 2022, 13(8):750
Front Oncol, 2020, 10;10:331
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
S2300 Ferulic Acid Ferulic Acid (Fumalic) is a hydroxycinnamic acid and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong. Ferulic acid is a novel fibroblast growth factor receptor (FGFR) inhibitor with IC50s of 3.78 μM and 12.5 μM for FGFR1 and FGFR2, respectively.
Pharm Biol, 2022, 60(1):2286-2294
J Med Virol, 2019, 91(8):1440-1447
Biomed Pharmacother, 2019, 120:109482
S6539 ASP5878 ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.
J Biol Chem, 2021, S0021-9258(21)00950-9
bioRxiv, 2020, 10.1101/2020.05.20.107326
bioRxiv, 2020, 10.1101/2020.05.20.107326
S9031 Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
Chem Biol Interact, 2023, 382:110602
Oncotarget, 2021, 12(6):549-561
Cancer Lett, 2020, 469:277-286
S8548 Roblitinib (FGF401) FGF401 is an FGFR4-selective inhibitor with an IC50 of 1.9 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays.
J Exp Clin Cancer Res, 2023, 42(1):96
Br J Cancer, 2022, 10.1038/s41416-022-01973-6
Front Oncol, 2022, 12:936952
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
S8754 Alofanib (RPT835) Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
Cell Death Dis, 2022, 13(8):724
JCI Insight, 2022, e157874
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
S7940 NSC12 NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.
Biomed Pharmacother, 2018, 107:359-367
S8404 S49076 S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.
Mol Brain, 2020, 4;13(1):66
S8578 PRN1371 PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.
Nat Commun, 2021, 12(1):6572
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
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.
E4474New Infigratinib Phosphate Infigratinib Phosphate (NVP-BGJ398 phosphate) is the phosphate salt form of infigratinib, an orally bioavailable pan-inhibitor of human fibroblast growth factor receptors (FGFRs) with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively. It also has potential antiangiogenic, antineoplastic and antitumor activities.
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.
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.
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.
S8965 BO-264 BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.
E1431New Lirafugratinib Lirafugratinib (RLY-4008) is an orally active and selective inhibitor of FGFR2.
S7715 FIIN-3 FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, 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).
S8192 SUN11602 SUN11602 is a small synthetic compound that mimics the neuroprotective activities of bFGF and activates key molecules in the FGF receptor-1-mitogen-activated protein kinase/extracellular signal-regulated kinase-1/2 kinase (FGFR-1-MEK/ERK) signaling pathway.
E4474New Infigratinib Phosphate Infigratinib Phosphate (NVP-BGJ398 phosphate) is the phosphate salt form of infigratinib, an orally bioavailable pan-inhibitor of human fibroblast growth factor receptors (FGFRs) with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively. It also has potential antiangiogenic, antineoplastic and antitumor activities.
E1431New Lirafugratinib Lirafugratinib (RLY-4008) is an orally active and selective inhibitor of FGFR2.
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).

FGFR阻害剤の選択性比較

Tags: FGFR inhibition | FGFR signaling | FGFR pathway | FGFR phosphorylation | FGFR activation | FGFR inhibitors clinical trials | FGFR inhibitor review