GNE-049 ( GNE049;GNE 049 )

产品货号. M13034 CAS No. 1936421-41-8

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

GNE-049
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.
产品描述

GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively; displays 3,850-fold selectivity over BRD4; shows excellent potency (12 nM) in a BRET cellular assay and inhibits the expression of MYC with EC50 of 14 nM in MV-4-11 cells; demonstrates significant dose-dependent inhibition of AR signaling and PC proliferation in vitro and in vivo.
同义词

GNE049;GNE 049
通路

Chromatin/Epigenetic
靶点

Bromodomain
受体

Bromodomain
研究领域

——
适应症

——

CAS Number

1936421-41-8
分子量

510.59
分子式

C27H32F2N6O2
纯度

>98% (HPLC)
溶解度

DMSO : 100 mg/mL 195.86 mM
SMILES

CC(N1CCC(N(C2COCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)=O
化学全称

1-(3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethan-1-one