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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-BET inhibitor CF53
BET inhibitor CF53

Chemical Structure : BET inhibitor CF53

CAS No.: 1808160-52-2

BET inhibitor CF53 (CF53)

货号: PC-35401Not For Human Use, Lab Use Only.

BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1).

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

生物&药学活性

BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1).
BET inhibitor CF53 potently inhibits different BET proteins with Kd values of 0.5-2.2 nM, weakly inhibits CREBBP (Ki=47 nM) and shows excellent selectivity over other bromodomain containing proteins.
BET inhibitor CF53 inhibits cell growth in MOLM-13 and MDA-MB-231 cell lines with IC50 of 7 and 85 nM, respectively.
CF53 demonstrates significant antitumor activity in both triple-negative breast cancer and acute leukemia xenograft models in mice.

物理化学性质&存储条件

分子量 443.511
分子式 C24H25N7O2
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

N-(3-Cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-2-methyl-9H-pyrimido[4,5-b]indol-4-amine

参考文献

1. Zhao Y, et al. J Med Chem. 2018 Jul 17. doi: 10.1021/acs.jmedchem.8b00483.

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