MPC-0767

MPC-0767 is an orally active prodrug of Hsp90 inhibitor. MPC-0767 undergoes rapid biotransformation to the parent Hsp90 inhibitor MPC-3100 via enzyme-mediated luminal cleavage. MPC-0767 is applicable to the research of refractory and recurrent cancers^[2]. In Vitro:MPC-0767 mesylate salt has a half-life of <2 min in mouse plasma, 300 min in monkey plasma, 149 min in human plasma, and 145 min in pH 7.4 phosphate buffer^[1].
MPC-0767 mesylate salt has a half-life of <2 min in mouse liver microsomes and 2 min in human liver microsomes, with no difference observed between assays run with or without NADPH^[1].
MPC-0767 mesylate salt is highly stable in simulated gastric fluid but undergoes rapid conversion in pancreatin-containing simulated intestinal fluid with a half-life of 22 min^[1]. In Vivo:MPC-0767 mesylate salt (p.o.; 265 mg/kg; single dose) exhibits superior pharmacokinetic properties^[1].

MPC-0767 mesylate salt (p.o.; 265 mg/kg) exhibits comparable efficacy in the N-87 xenograft tumor model, inducing a 46% reduction in tumor volume without causing body weight loss^[1].