fakin1

FAK-IN-1, a FAK inhibitor with anticancer activities (WO2020231726 [Example 27]).

OXA-11 (FAK-IN-16) is an orally active, selective focal adhesion kinase (FAK) inhibitor with antitumor activity. It inhibits FAK phosphorylation at tyrosine 397 in a dose-dependent manner and suppresses TOV21G tumor growth. It is used in cancer research.

FAK-IN-17 is an inhibitor of focal adhesion kinase (FAK). It exhibits anticancer properties with IC50 values of 130 nM in A549 cells and 94 nM in MDA-MB-231 cells.

FAK-IN-10 is an inhibitor of FAK (IC50: 76.3 μM) and demonstrates antitumor activity in MCF-7 and A431 cell lines with IC50 values of 4.23 μM and 0.78 μM, respectively.

FAK-IN-14 is a highly effective focal adhesion kinase (FAK) inhibitor that induces apoptosis and cell cycle arrest. FAK-IN-14 has weak inhibitory effects on Akt, c-kit, MEK1/2 and mTOR, but has significant inhibitory effects on FAK, FGFR1 and Pyk2.

FAK-IN-15 is a highly potent focal adhesion kinase (FAK) inhibitor with antitumor activity.

FAK-IN-11 (Compound 4l), a FAK inhibitor, specifically targets the ATP binding pocket of FAK to prevent its phosphorylation. It exhibits cytotoxic effects on MDA-MB-231 cells, achieving an IC50 value of 13.73 μM, and induces non-apoptotic cell death in these cells [1].

FAK-IN-12 (Compound 12S) is a selective FAK inhibitor with an IC50 of 47 nM, effectively suppressing proliferation of MGC-803, HCT-116, and KYSE30 cells with IC50 values of 0.24, 0.45, and 0.44 μM, respectively. Additionally, FAK-IN-12 promotes apoptosis and cellular senescence [1].

FAK-IN-19 (ligand3), an inhibitor co-crystallized with FAK, exhibits anticancer effects [1].