SK-575

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。

SK-575 

SK-575 是一种高效、特异的蛋白水解靶向嵌合体 (PROTAC) 的 PARP1 降解剂。SK-575 能有效抑制携带 BRCA1/2 突变的癌细胞的生长。SK-575 抑制 MDA-MB-436 和 Capan-1 细胞生长,IC50 值分别为 19±6 nM 和 56±12 nM。

SK-575

SK-575 Chemical Structure

CAS No. : 2523016-96-6

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生物活性

SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations. SK-575 inhibits cell growth in MDA-MB-436 and Capan-1 cells, with IC50 values of 19 ± 6 nM and 56 ± 12 nM, respectively[1].

IC50 & Target

PARP1

 

体内研究
(In Vivo)

SK-575 achieves sufficient exposure in plasma for over 24 h and effectively induces PARP1 degradation in the SW620 xenograft tumor tissue with the effect persisting for >24 h[1].
SK-575 (mice bearing BRCA2-mutated Capan-1 xenografts, 25 and 50 mg/kg, IP, once daily for 5 days) significantly inhibits the tumor growth in vivo as a single-agent in HR-deficient xenograft models[1].

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

分子量

876.97

Formula

C47H53FN8O8

CAS 号

2523016-96-6

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]. Cao C, et al. Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. J Med Chem. 2020 Oct 8;63(19):11012-11033.

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