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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-Lerzeparib
Lerzeparib

Chemical Structure : Lerzeparib

CAS No.: 2459693-01-5

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Lerzeparib (TQB-3823,TQB3823)

货号: PC-23088Not For Human Use, Lab Use Only.

Lerzeparib (TQB3823) is a novel, potent and selective PARP inhibitor with IC50 of  2.8/0.9/629.3 nM for PARP1/PARP2/Tankyrase 1, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Lerzeparib (TQB3823) is a novel, potent and selective PARP inhibitor with IC50 of  2.8/0.9/629.3 nM for PARP1/PARP2/Tankyrase 1, respectively.
Lerzeparib (TQB3823) inhibits proliferation of BRCA1 mutant MDA-MB-436 cell with IC50 of 9.6 nM, shows little anti-proliferative activity in BRCA-wild type MDA-MB-231 cell with IC50 >10 μM. 
Lerzeparib (TQB3823) demonstrated antitumor efficacy in dose dependent fashions with tumor regression was observed at 25 mg/kg in MDA-MB-436 CDX model. 

物理化学性质&存储条件

分子量 365.41
分子式 C21H20FN3O2
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

8-Fluoro-1,3-dihydro-2-[4-[(2R)-2-methyl-2-pyrrolidinyl]phenyl]pyrrolo[4,3,2-ef][3,2]benzoxazepin-6(5H)-one

参考文献

1. Hu Yanbin, et al. Cancer Res (2021) 81 (13_Supplement): 2054.

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