| S7654 |
Defactinib (VS-6063)
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Defactinib (VS-6063, PF-04554878) is a selective, orally active FAK inhibitor currently in Phase 2.
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Nat Commun, 2025, 16(1):4581
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Adv Sci (Weinh), 2025, 12(44):e11726
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Cell Death Dis, 2025, 16(1):34
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| S2890 |
PF-562271 (VS-6062)
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PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
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Cell Death Differ, 2025, 10.1038/s41418-025-01469-9
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Front Oncol, 2025, 15:1498005
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Cell Rep, 2024, 43(12):114992
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| S2013 |
PF-573228
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PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. This compound induces apoptosis.
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Nat Commun, 2025, 16(1):7287
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Nat Commun, 2025, 16(1):2254
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Cell Rep Med, 2025, 6(2):101943
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| S7653 |
VS-4718 (PND-1186)
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VS-4718 (PND-1186) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM, which selectively promotes tumor cell apoptosis. Phase 1.
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Cell Death Differ, 2025, 10.1038/s41418-025-01469-9
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Front Immunol, 2025, 16:1596802
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iScience, 2025, 28(1):111564
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| S7357 |
PF-562271 HCl
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PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
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Nat Cardiovasc Res, 2023, 2(6):550-571
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Front Immunol, 2022, 13:837180
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Cancers (Basel), 2022, 14(6)1537
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| S2672 |
PF-562271 Besylate
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PF-562271 Besylate is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
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JCI Insight, 2025, 10(13)e187684
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Elife, 2023, 12RP89141
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Elife, 2023, 12RP89141
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| S2820 |
TAE226 (NVP-TAE226)
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TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. This compound induces apoptosis.
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Exp Ther Med, 2025, 29(5):93
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Theranostics, 2022, 12(3):1097-1116
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Proc Natl Acad Sci U S A, 2022, 119(32):e2201328119
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| S8523 |
GSK2256098
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GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. This compound inhibits cancer cell growth and induces apoptosis.
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Front Immunol, 2025, 16:1596802
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iScience, 2025, 28(4):112176
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Sci Rep, 2025, 15(1):20840
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| S7644 |
PF-431396
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PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
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bioRxiv, 2025, 2025.07.31.668026
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Cytojournal, 2024, 21:34
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Nat Commun, 2023, 14(1):6270
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| S5321 |
Y15
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Y15 (1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14) is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.
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Cell Commun Signal, 2025, 23(1):368
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Phytother Res, 2025, 10.1002/ptr.8519
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Commun Biol, 2025, 8(1):595
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