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PROTAC B-Raf degrader 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PROTAC B-Raf degrader 1图片
规格:98%
分子量:763.77
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
PROTAC B-Raf degrader 1 (compound 2) 是基于 Cereblon 配体的一种 B-Raf PROTAC。有抗肿瘤活性。
货号:ajcx39660
CAS:2364367-27-9
分子式:C36H37N5O12S
分子量:763.77
溶解度:DMSO : 25 mg/mL (32.73 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity[1].

The IC50 values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM, respectively[1].PROTAC B-Raf degrader 1 (5 or 10 μM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf[1].MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 μM[1].PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase[1].

[1]. Chen H, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Mar 19;87:191-199.

Protocol:

B-Raf