CH6953755 is a potent, orally active and selective inhibitor of YES1 kinase (IC50: 1.8 nM). It inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.

CH6953755 (0.001-1 μM; for 2 hours) prevents the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification. CH6953755 (0.001-1 μM; for 4 days) inhibits the cell growth of YES1-amplified cancer cell lines. CH6953755 (0.1, 0.3, 1, 3 μM) suppresses TEAD luciferase reporter activity in YES1-amplified KYSE70 and RERF-LC-AI.

CH6953755 (p.o.; 7.5, 15, 30, 60 mg/kg) suppresses phospho-Tyr426 YES1 in a dose-dependent manner. CH6953755 (p.o.; 60 mg/kg/day; for 10 days) shows selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors.

2055918-71-1

C26H22F2N6O4S

552.55

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years