MPC-0767

MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester prodrug of MPC-3100 with improved chemical stability[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HSP

Signaling Pathways >> Cell Cycle/DNA Damage >> HSP

HSP90

MPC-0767 (oral adminstration; 265 mg/kg; single dose) exhibits a improved PK property, the Tmax, Cmax, AUC and F% are 1 (h), 21562 ng/mL, 94194 h*ng/mL and 56%, respectively[1]. MPC-0767 (oral adminstration; 265 mg/kg) demonstrates comparable efficacy in an N-87 xenograft tumor model, the 46% tumor size reduction with no evidence of weight loss in the study animals[1]. MPC-0767 is well tolerated when administered at 252 mg/kg po (equivalent to 200 mg/kg dose of MPC-3100)[1].

[1]. Se-Ho Kim, et al. Discovery of an L-alanine ester prodrug of the Hsp90 inhibitor, MPC-3100. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5254-7.