FAK inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S7654 Defactinib (VS-6063) Defactinib (VS-6063, PF-04554878) is a selective, orally active FAK inhibitor currently in Phase 2.
Nat Commun, 2025, 16(1):4581
Adv Sci (Weinh), 2025, 12(44):e11726
Cell Death Dis, 2025, 16(1):34
Verified customer review of Defactinib (VS-6063)
S2890 PF-562271 (VS-6062) 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.
Cell Death Differ, 2025, 10.1038/s41418-025-01469-9
Front Oncol, 2025, 15:1498005
Cell Rep, 2024, 43(12):114992
Verified customer review of PF-562271 (VS-6062)
S2013 PF-573228 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.
Nat Commun, 2025, 16(1):7287
Nat Commun, 2025, 16(1):2254
Cell Rep Med, 2025, 6(2):101943
Verified customer review of PF-573228
S7653 VS-4718 (PND-1186) 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.
Cell Death Differ, 2025, 10.1038/s41418-025-01469-9
Front Immunol, 2025, 16:1596802
iScience, 2025, 28(1):111564
Verified customer review of VS-4718 (PND-1186)
S7357 PF-562271 HCl 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.
Nat Cardiovasc Res, 2023, 2(6):550-571
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
Verified customer review of PF-562271 HCl
S2672 PF-562271 Besylate 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.
JCI Insight, 2025, 10(13)e187684
Elife, 2023, 12RP89141
Elife, 2023, 12RP89141
Verified customer review of PF-562271 Besylate
S2820 TAE226 (NVP-TAE226) 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.
Exp Ther Med, 2025, 29(5):93
Theranostics, 2022, 12(3):1097-1116
Proc Natl Acad Sci U S A, 2022, 119(32):e2201328119
Verified customer review of TAE226 (NVP-TAE226)
S8523 GSK2256098 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.
Front Immunol, 2025, 16:1596802
iScience, 2025, 28(4):112176
Sci Rep, 2025, 15(1):20840
S7644 PF-431396 PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
bioRxiv, 2025, 2025.07.31.668026
Cytojournal, 2024, 21:34
Nat Commun, 2023, 14(1):6270
S5321 Y15 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.
Cell Commun Signal, 2025, 23(1):368
Phytother Res, 2025, 10.1002/ptr.8519
Commun Biol, 2025, 8(1):595

Signaling Pathway Map