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GNE-049

Chemical Structure : GNE-049

CAS No.: 1936421-41-8

GNE-049 (GNE049;GNE 049)

货号: PC-61641Not For Human Use, Lab Use Only.

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

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.
GNE-049 displays 3,850-fold selectivity over BRD4.
GNE-049 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.
GNE-049 demonstrates significant dose-dependent inhibition of AR signaling and PC proliferation in vitro and in vivo.

物理化学性质&存储条件

分子量 510.59
分子式 C27H32F2N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Jin L, et al. Cancer Res. 2017 Aug 17. pii: canres.0314.2017.

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