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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-CZL-077
CZL-077

Chemical Structure : CZL-077

CAS No.: 3032444-06-4

CZL-077 (CZL077)

货号: PC-25946Not For Human Use, Lab Use Only.

CZL-077 is a potent, selective and orally active p300/CBP bromodomain inhibitor with IC50 of 34 nM and 52 nM respectively, selective over BRD4 BD1 and BD2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CZL-077 is a potent, selective and orally active p300/CBP bromodomain inhibitor with IC50 of 34 nM and 52 nM respectively, selective over BRD4 BD1 and BD2.
CZL-077 effectively inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively.
CZL-077 exhibits high selectivity over the BRDs of BET proteins.
CZL-077 shows potent in vivo efficacy in the OPM-2 xenograft model and demonstrates more potent antitumor activity in the 22RV1 xenograft model, with tumor growth inhibition values of 56.2% and 72.8%, respectively

物理化学性质&存储条件

分子量 577.63
分子式 C30H26F3N5O2S
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

(3S,5S)-1-(3,4-difluorophenyl)-5-(5-(3,5-dimethylisoxazol-4-yl)-1-((R)-2-methyl-4,5,6,7-tetrahydrobenzo[d]thiazol-6-yl)-1H-benzo[d]imidazol-2-yl)-3-fluoropyrrolidin-2-one

参考文献

1. Chen Z, et al. Eur J Med Chem. 2025 Dec 16;304:118489.

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