产品名称

Mivebresib(ABBV-075)

一般描述

Mivebresib(ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM 54-fold selectivity vs. BRD4).

别 称

N-[4-(2,4-difluorophenoxy)-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide

纯 度

≥98.5%(HPLC)

CAS NO.

1445993-26-9

分子式

C²²H¹⁹F²N³O⁴S

分子量

459.47

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25°C)

DMSO

≥50mg/ml

乙醇

Insoluble

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

Mivebresib is an inhibitor of one or more as of yet undisclosed bromodomain (BRD)-containing protein(s), with potential antineoplastic activity. Upon administration, mivebresib binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the  of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors.

l  存储

存储温度

-20°C

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov