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ARV-825
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。
ARV-825图片
CAS NO:1818885-28-7
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
ARV-825 是一种双功能 PROTAC,蛋白水解靶向嵌合体,将 BRD4 募集到 E3 泛素连接酶大脑中,导致 BRD4 在所有测试的 BL 细胞系中快速、有效和延长降解。对 BRD4 的 BD1 和 BD2 结构域具有高亲和力,Kd值分别为 90 和 28 nM。

产品描述

ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.

体外活性

ARV-825 more effectively suppresses c-MYC levels and downstream signaling than small molecule BRD4 inhibitors resulting in more effective cell proliferation inhibition and apoptosis induction in BL.In Burkitt's lymphoma cells, ARV-825 reduces c-Myc levels, blocks cell proliferation, and induces apoptosis.

细胞实验

Cells (50000/100ul) were seeded in 96-well tissue culture plates followed by addition of ARV-825?at indicated concentration.?After 72 hours, 100 μL per well of reconstituted CellTiter-Glo reagent was added and read on Cytation 3 imaging reader.?Relative cell growth was determined by comparing assay readings of treated cells with control DMSO treated cells.?For apoptosis induction, Caspase-Glo 3/7 Assay was used following manufacturer s instruction.

Cas No.

1818885-28-7

分子式

C46H47ClN8O9S

分子量

923.44

储存和溶解度

DMSO:50 mg/mL (54.15 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years