| S2183 |
BGJ398 (Infigratinib)
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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.
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Adv Healthc Mater, 2025, e04817.
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Cancer Lett, 2025, 619:217668
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JCI Insight, 2025, 10(21)e184863
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| S1264 |
PD173074
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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.
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Stem Cell Reports, 2025, 20(10):102640
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Commun Biol, 2025, 8(1):125
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Cell Stem Cell, 2024, S1934-5909(24)00294-7
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| S8401 |
Erdafitinib (JNJ-42756493)
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Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. This compound also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.
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Commun Biol, 2025, 8(1):394
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Int J Mol Sci, 2025, 26(8)3525
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J Clin Invest, 2024, 134(2)e169241
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| S1490 |
Ponatinib (AP24534)
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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.
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Nat Commun, 2025, 16(1):471
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Theranostics, 2025, 15(8):3589-3609
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J Exp Clin Cancer Res, 2025, 44(1):290
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| S1010 |
BIBF 1120 (Nintedanib)
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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.
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Nat Commun, 2025, 16(1):471
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Cell Death Dis, 2025, 16(1):196
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Eur J Pharmacol, 2025, 1005:178058
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| S1164 |
E7080 (Lenvatinib)
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Lenvatinib 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.
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Nature, 2025, 10.1038/s41586-025-08585-z
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Drug Resist Updat, 2025, 81:101224
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Nat Cancer, 2025, 10.1038/s43018-025-01058-2
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| S7667 |
SU5402
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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.
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Int J Mol Sci, 2025, 26(8)3536
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Basic Clin Pharmacol Toxicol, 2025, 136(5):e70022
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Sci Adv, 2025, 11(30):eadi2370
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| S8161 |
ON123300
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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.
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Cell Rep Med, 2025, S2666-3791(25)00231-9
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Cell Rep, 2024, 43(7):114446
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J Cell Sci, 2021, jcs.258685
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| S2801 |
Fexagratinib (AZD4547)
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Fexagratinib (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.
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Nat Cancer, 2025, 6(1):67-85
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Nat Commun, 2025, 16(1):4128
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Theranostics, 2025, 15(18):9399-9414
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| S7819 |
BLU9931
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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.
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Kidney Int, 2025, S0085-2538(25)00087-0
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JCI Insight, 2024, 9(15)e174888
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J Cardiovasc Dev Dis, 2024, 11(10)320
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