产品描述:
RGB-286638 is a multi-kinase inhibitor.{47793} It inhibits a variety of kinases, including cyclin-dependent kinase 1 (CDK1), CDK2-7 and CDK9, as well as the tyrosine kinases FMS, JAK2, and c-Src and the serine/threonine kinases GSK3β, TAK1, JNK1A1, JNK1A2, AMPK, and MEK1 (IC50s = 1-55 nM). RGB-286638 inhibits proliferation of multiple myeloma cancer cell lines endogenously expressing mutant and wild-type p53 (EC50s = 20-70 nM), as well as patient-derived multiple myeloma cells when used at concentrations of 50 and 100 nM. It induces G1/S and G2/M cell cycle arrest and apoptosis of MM.1S human multiple myeloma cells when used at a concentration of 50 nM. RGB-286638 decreases tumor growth in an MM.1S mouse xenograft model when administered at doses of 30 and 40 mg/kg per day for 14 days.