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FAK Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
E1114 Ifebemtinib (IN10018, BI-853520) Ifebemtinib(IN10018, BI853520) is a highly selective, potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM for inhibiting FAK autophosphorylation. It also inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively, inhibiting spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. IN10018 exhibits anti-tumor activity in vitro and in vivo.
E1783 Conteltinib(CT-707) 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.
E0806 Narmafotinib Narmafotinib (AMP-945) is an inhibitor of focal adhesion kinase (FAK).
E3677 Semen Ziziphi Spinosae Extract Semen Ziziphi Spinosae Extract is extracted from the seeds of Semen Ziziphi Spinosae, which can attenuate blood-brain barrier dysfunction induced by lipopolysaccharide by targeting the FAK-DOCK180-Rac1-WAVE2-Arp3 signaling pathway.
E1113 GSK215 GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader, which exerts FAK degradation in A549 non-small-cell lung cancer cells with DC50 of 1.3 nM by a strong time-dependence way and maximal degradation (Dmax) near the limit of the assay quantification (Dmax 99%).
E7468 Defactinib hydrochloride Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is an inhibitor of FAK. It inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. This compound overcomes YB-1-mediated paclitaxel resistance via AKT-dependent pathway in ovarian cancer.
S2360 Solanesol (Nonaisoprenol) Solanesol (Nonaisoprenol, Betulanonaprenol) is a long-chain polyisoprenoid alcohol compound with inhibitory activities toward FAK. It mainly accumulates in solanaceous crops, including tobacco, tomato, potato, eggplant, and pepper plants.
S8032 PRT062607 (P505-15) HCl 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.
Sci Adv, 2025, 11(31):eadu4270
Sci Rep, 2024, 14(1):7739
J Exp Med, 2023, 220(9)e20230054
Verified customer review of PRT062607 (P505-15) HCl
E1961 NVL-655 (Neladalkib) 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.
Pharm Res, 2025, 42(9):1497-1509
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM.
E1508 APG-2449 APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. This compound exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models.
E0814 Masitinib mesylate Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK.