OARV-771

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。

OARV-771 

OARV-771 是一种基于 VHL 的 BET 降解剂 (PROTAC),具有改善的细胞通透性。OARV-771 显示 Brd4、Brd2 和 Brd3 的 DC50 分别为 6、1 和 4 nM。

OARV-771

OARV-771 Chemical Structure

CAS No. : 2683008-37-7

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生物活性

OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively[1].

IC50 & Target[1]

BRD4

6 nM (DC50)

BRD2

1 nM (DC50)

BRD3

4 nM (DC50)

VHL

 

体外研究
(In Vitro)

OARV-771 shows antiproliferative effect with an EC50 value of 4 nM in MV4;11[1].

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

分子量

987.62

Formula

C49H59ClN8O8S2

CAS 号

2683008-37-7

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]. Klein VG, et al. Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. J Med Chem. 2021;64(24):18082-18101.

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