MPC-0767

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

MPC-0767 

MPC-0767 是一种有效的、选择性的、口服的 hsp90 抑制剂。MPC-0767 是 MPC-3100 的 L-丙氨酸酯前药,化学稳定性提高。

MPC-0767

MPC-0767 Chemical Structure

CAS No. : 1310540-32-9

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生物活性

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].

IC50 & Target

HSP90

 

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

734.64

Formula

C26H36BrN7O9S2

CAS 号

1310540-32-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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