Chiauranib (Ibcasertib, CS2164) is a potent multi-kinase inhibitor, inhibits VEGFR2, Aurora B and CSF‐1R kinases with IC50 values of 7, 9 and 7 nM, respectively.
CS2164 interacts with each active ATP‐binding pocket of VEGFR2, Aurora B and CSF‐1R kinases, respectively.
CS2164 also displays inhibitory activities with single digital nanomolar IC50 against several angiogenesis‐related kinases, including VEGFR1, VEGFR3, PDGFRα and c‐Kit.
CS2164 only shows moderate inhibitory activities (100 nM < IC50 < 500 nM) in 4 kinases (c‐RAF, DDR2, PLK1 and PLK3), little activity (IC50 > 500 nM) in 33 kinases, and almost no activity (IC50 > 10 μM) in over 120 kinases, including 76 GPCR and 8 ion channels tested.
CS2164 potently inhibits VEGF‐induced proliferation of HUVEC cells and PDGF‐induced proliferation of NIH‐3T3 cells with GI50 values of 20.70 and 44.16 nM, respectively.
CS2164 is a potent inhibitor of tumor angiogenesis through targeting the corresponding tyrosine receptor signaling pathways, induces G2/M cell cycle arrest by inhibition of Aurora B/p‐H3.
CS2164 inhibits CSF‐1R signaling and reduces tissue CSF‐1R expression.
CS2164 exhibits broad and potent in vivo anti‐tumor activities, CS2164 (40 mg/kg) induces dose‐dependent inhibition of tumor growth in human non‐small cell lung cancer cell line A549‐derived xenograft model.