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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-CZL-046
CZL-046

Chemical Structure : CZL-046

CAS No.: 3032444-02-0

CZL-046 (CZL046)

货号: PC-23754Not For Human Use, Lab Use Only.

CZL-046 is a potent, selective, and orally active p300 bromodomain inhibitor with IC50 of 3.3 nM, exhibits antiproliferative activity in the multiple myeloma (MM) cell line (OPM-2, IC50=51.5 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CZL-046 is a potent, selective, and orally active p300 bromodomain inhibitor with IC50 of 3.3 nM, exhibits antiproliferative activity in the multiple myeloma (MM) cell line (OPM-2, IC50=51.5 nM).
CZL-046 shows slightly higher selectivity over the bromodomains of BET proteins than CCS1477, especially BD2 with IC50 values greater than 9 μM.
CZL-046 suppresses the mRNA levels of c-Myc and IRF4 and downregulated the expression of c-Myc and H3K27Ac, exhibits intracellular H3K27Ac inhibitory activity with IC50 of 109 nM in OPM-2 cell line.
CZL-046 induces apoptosis and cell cycle G0/G1 phase arrest in OPM-2 cells
CZL-046 significantly inhibited the growth of the tumor with 30 mg/kg oral administration following 21 days of once-daily dosing in OPM-2 xenograft model.

物理化学性质&存储条件

分子量 541.59
分子式 C29H26D3F3N4O3
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-((1r,4S)-4-(methoxy-d3)cyclohexyl)-1H-benzo[d]imidazole-2-yl)-3-fluoropyrrolidin-2-one

参考文献

1. Chen Z, et al. J Med Chem. 2024 Oct 24;67(20):18606-18628.

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