CH6953755 (CH 6953755) is a potent, selective, orally available YES1 kinase inhibitor with IC50 of 1.8 nM.
CH6953755 exhibits good specificity for YES1 among the tested Src family kinases (SFKs), inhibits 8/456 WT and mutant kinases at 10 nM (>60% inhibition) including YES1 and four other SFKs.
CH6953755 inhibits cell growth inhibition of YES1-amplified cancer cell lines.
CH6953755 shows selective antitumor activity against YES1-amplified xenograft tumors.
CH6953755 inhibits YAP1 nuclear localization, neither the YAP1 Y357E nor the Y357F mutation affected the suppression of YAP1 transcriptional activity by CH6953755.
YES1-YAP1 signal inhibition by CH6953755 leads to antitumor activity in YES1-amplified cancer cells.
