CHMFL-BMX-078

CHMFL-BMX-078 is a potent and selective type II irreversible inhibitor of Bone Marrow Kinase in the X chromosome (BMX, also known as ETK). It functions by forming a covalent bond with the Cys496 residue in the DFG-out inactive conformation of the kinase. With an IC50 of 11 nM, it exhibits high kinome selectivity, including over 40-fold selectivity against the closely related Bruton's tyrosine kinase (BTK). Preclinical research indicates that CHMFL-BMX-078 can overcome vemurafenib resistance in melanoma by inhibiting the AKT signaling pathway and demonstrates antiproliferative activity in BMX-dependent cell lines. Due to its poor oral bioavailability and short half-life (0.80 h), it is typically administered via intravenous or intraperitoneal injection in experimental models.

Other names

2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamideCAS 1808288-51-8CAS1808288-51-8CAS-1808288-51-8