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Catalog No. Product Name Information Product Use Citations Product Validations
S0088 Pemigatinib (INCB054828) Pemigatinib (INCB054828, Pemazyre) 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 Res, 2021, canres.0955.2021
Cell Death Differ, 2021, 10.1038/s41418-021-00897-7
Cancer Med, 2021, 10.1002/cam4.4041
S0487 Sulfatinib Sulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib) 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.
S1010 Nintedanib (BIBF 1120) Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 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.
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cell Rep, 2021, 34(12):108882
Cancers (Basel), 2021, 13(16)4168
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.
Mol Cell, 2021, S1097-2765(21)00507-4
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancer Res, 2021, canres.1780.2020
S1035 Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 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.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(14)3635
J Clin Endocrinol Metab, 2021, dgab020
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) 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.
Cancer Cell, 2021, S1535-6108(21)00659-0
Leukemia, 2021, 10.1038/s41375-021-01308-z
Theranostics, 2021, 11(12):5650-5674
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.
J Cell Physiol, 2020, 235(2):1259-1273
Mol Pharm, 2019, 16(11):4436-4450
Eur J Cancer, 2016, 61:20-8
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.
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
Mol Cell, 2020, 80(6):1104-1122.e9
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
S1164 Lenvatinib (E7080) Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.
Nature, 2021, 595(7869):730-734
Cancer Cell, 2021, S1535-6108(21)00659-0
Hepatology, 2021, 10.1002/hep.31921
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
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.
Adv Sci (Weinh), 2021, 8(2):2002922
Nat Commun, 2021, 12(1):3017
EMBO J, 2021, e107182
S1490 Ponatinib (AP24534) Ponatinib (AP24534) 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.
J Ethnopharmacol, 2022, 283:114667
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Mol Syst Biol, 2021, 17(9):e10426
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.
Nature, 2021, 10.1038/s41586-020-03085-8
Nature, 2021, 595(7869):730-734
Cancer Cell, 2021, S1535-6108(21)00492-X
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.
Biomed Pharmacother, 2019, 120:109482
J Med Virol, 2019, 91(8):1440-1447
J Nutr Biochem, 2015, 26(11):1379-84
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
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.
Nature, 2021, 595(7869):730-734
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Sci Adv, 2021, 7(7)eabd2645
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 Res, 2021, canres.1222.2021
Cancers (Basel), 2021, 13(14)3635
Radiother Oncol, 2021, 157:175-181
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.
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancers (Basel), 2021, 13(16)4168
Cell Death Dis, 2021, 12(10):947
S5240 Lenvatinib (E7080) Mesylate Lenvatinib Mesylate (E7080) 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.
J Immunother Cancer, 2021, 9(6)e002305
Cancer Lett, 2021, 519:46-62
Cancers (Basel), 2021, 13(11)2539
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.
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
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.
Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118
Am J Cancer Res, 2020, 10(11):3765-3783
Protein Cell, 2019, 10(3):161-177
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
S7647New 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.
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.
J Cell Physiol, 2021, 10.1002/jcp.30657
Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104
Elife, 2019, 8
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.
Nature, 2021, 10.1038/s41586-020-03085-8
Nat Commun, 2021, 12(1):2551
Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118
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.
Front Oncol, 2020, 10;10:331
Front Oncol, 2019, 9:179
Front Oncol, 2019, 9:179
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258, CHIR258) Lactate 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
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.
Breast Cancer Res, 2021, 23(1):82
Aging (Albany NY), 2021, 13(2):2982-3009
Oncogene, 2020, 39(17):3507-3521
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
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.
J Cardiovasc Dev Dis, 2021, 8(3)28
Mol Med Rep, 2021, 23(4):1
CellPress, 2021, None
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
S8401 Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493) 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.
Nature, 2021, 10.1038/s41586-020-03085-8
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
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
S8493 PD-166866 (PD166866) 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.
Cell Rep, 2021, 35(11):109233
Oxid Med Cell Longev, 2021, 2021:8996482
Histochem Cell Biol, 2021, 156(3):227-237
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.
Nature, 2021, 595(7869):730-734
Cancer Res, 2020, canres.1992.2020
Cancers (Basel), 2020, 12(8):E2010
S8548 Roblitinib (FGF401) Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.1 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.
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
S8609 Derazantinib(ARQ-087) Derazantinib(ARQ-087) 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.
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).
J Exp Clin Cancer Res, 2021, 40(1):93
NPJ Precis Oncol, 2021, 5(1):66
Thorac Cancer, 2018, 9(12):1687-1698
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.
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 Res, 2021, canres.1780.2020
Oncogenesis, 2021, 10(7):55
Cancer Med, 2021, 10.1002/cam4.4041
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.
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.
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.
Oncotarget, 2021, 12(6):549-561
Cancer Lett, 2020, 469:277-286
A5086 FGFR1 Rabbit Recombinant mAb FGFR1 Rabbit Recombinant mAb detects endogenous levels of FGFR1.
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.
S0088 Pemigatinib (INCB054828) Pemigatinib (INCB054828, Pemazyre) 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 Res, 2021, canres.0955.2021
Cell Death Differ, 2021, 10.1038/s41418-021-00897-7
Cancer Med, 2021, 10.1002/cam4.4041
S0487 Sulfatinib Sulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib) 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.
S1010 Nintedanib (BIBF 1120) Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 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.
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cell Rep, 2021, 34(12):108882
Cancers (Basel), 2021, 13(16)4168
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.
Mol Cell, 2021, S1097-2765(21)00507-4
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancer Res, 2021, canres.1780.2020
S1035 Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 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.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(14)3635
J Clin Endocrinol Metab, 2021, dgab020
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) 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.
Cancer Cell, 2021, S1535-6108(21)00659-0
Leukemia, 2021, 10.1038/s41375-021-01308-z
Theranostics, 2021, 11(12):5650-5674
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.
J Cell Physiol, 2020, 235(2):1259-1273
Mol Pharm, 2019, 16(11):4436-4450
Eur J Cancer, 2016, 61:20-8
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.
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
Mol Cell, 2020, 80(6):1104-1122.e9
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
S1164 Lenvatinib (E7080) Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.
Nature, 2021, 595(7869):730-734
Cancer Cell, 2021, S1535-6108(21)00659-0
Hepatology, 2021, 10.1002/hep.31921
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
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.
Adv Sci (Weinh), 2021, 8(2):2002922
Nat Commun, 2021, 12(1):3017
EMBO J, 2021, e107182
S1490 Ponatinib (AP24534) Ponatinib (AP24534) 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.
J Ethnopharmacol, 2022, 283:114667
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Mol Syst Biol, 2021, 17(9):e10426
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.
Nature, 2021, 10.1038/s41586-020-03085-8
Nature, 2021, 595(7869):730-734
Cancer Cell, 2021, S1535-6108(21)00492-X
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.
Biomed Pharmacother, 2019, 120:109482
J Med Virol, 2019, 91(8):1440-1447
J Nutr Biochem, 2015, 26(11):1379-84
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
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.
Nature, 2021, 595(7869):730-734
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Sci Adv, 2021, 7(7)eabd2645
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 Res, 2021, canres.1222.2021
Cancers (Basel), 2021, 13(14)3635
Radiother Oncol, 2021, 157:175-181
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.
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Cancers (Basel), 2021, 13(16)4168
Cell Death Dis, 2021, 12(10):947
S5240 Lenvatinib (E7080) Mesylate Lenvatinib Mesylate (E7080) 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.
J Immunother Cancer, 2021, 9(6)e002305
Cancer Lett, 2021, 519:46-62
Cancers (Basel), 2021, 13(11)2539
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.
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
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.
Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118
Am J Cancer Res, 2020, 10(11):3765-3783
Protein Cell, 2019, 10(3):161-177
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
S7647New 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.
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.
J Cell Physiol, 2021, 10.1002/jcp.30657
Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104
Elife, 2019, 8
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.
Nature, 2021, 10.1038/s41586-020-03085-8
Nat Commun, 2021, 12(1):2551
Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118
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.
Front Oncol, 2020, 10;10:331
Front Oncol, 2019, 9:179
Front Oncol, 2019, 9:179
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258, CHIR258) Lactate 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
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.
Breast Cancer Res, 2021, 23(1):82
Aging (Albany NY), 2021, 13(2):2982-3009
Oncogene, 2020, 39(17):3507-3521
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
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.
J Cardiovasc Dev Dis, 2021, 8(3)28
Mol Med Rep, 2021, 23(4):1
CellPress, 2021, None
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
S8401 Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493) 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.
Nature, 2021, 10.1038/s41586-020-03085-8
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
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
S8493 PD-166866 (PD166866) 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.
Cell Rep, 2021, 35(11):109233
Oxid Med Cell Longev, 2021, 2021:8996482
Histochem Cell Biol, 2021, 156(3):227-237
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.
Nature, 2021, 595(7869):730-734
Cancer Res, 2020, canres.1992.2020
Cancers (Basel), 2020, 12(8):E2010
S8548 Roblitinib (FGF401) Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.1 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.
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
S8609 Derazantinib(ARQ-087) Derazantinib(ARQ-087) 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.
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).
J Exp Clin Cancer Res, 2021, 40(1):93
NPJ Precis Oncol, 2021, 5(1):66
Thorac Cancer, 2018, 9(12):1687-1698
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.
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 Res, 2021, canres.1780.2020
Oncogenesis, 2021, 10(7):55
Cancer Med, 2021, 10.1002/cam4.4041
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.
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.
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.
Oncotarget, 2021, 12(6):549-561
Cancer Lett, 2020, 469:277-286
A5086 FGFR1 Rabbit Recombinant mAb FGFR1 Rabbit Recombinant mAb detects endogenous levels of FGFR1.
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.
S7647New 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.
Tags: FGFR inhibition | FGFR signaling | FGFR pathway | FGFR phosphorylation | FGFR activation | FGFR inhibitors clinical trials | FGFR inhibitor review