| 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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| S8032 |
PRT062607 (P505-15) HCl
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PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
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Sci Adv, 2025, 11(31):eadu4270
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Sci Rep, 2024, 14(1):7739
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J Exp Med, 2023, 220(9)e20230054
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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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bioRxiv, 2023, 2023.06.02.543509
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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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| 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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| E1961 |
NVL-655 (Neladalkib)
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NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively.
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Pharm Res, 2025, 42(9):1497-1509
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| E1783 |
Conteltinib(CT-707)
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Conteltinib (CT-707), a potent multikinase inhibitor of ALK, FAK, and Pyk2, shows promising anti-tumor activities. It exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay.
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