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

Chemical Structure : Talazoparib

CAS No.: 1207456-01-6

Talazoparib (BMN-673, LT-673)

货号: PC-23876Not For Human Use, Lab Use Only.

Talazoparib (BMN-673) is a highly potent, selective PARP1/2 inhibitor (PARP1, IC50=0.57 nM), inhibits PARP1 and PARP2 to a similar extent with Ki of 1.20 and 0.85 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

Talazoparib (BMN-673) is a highly potent, selective PARP1/2 inhibitor (PARP1, IC50=0.57 nM), inhibits PARP1 and PARP2 to a similar extent with Ki of 1.20 and 0.85 nM, respectively.
Talazoparib (BMN-673) inhibits intracellular poly (ADP-ribose) (PAR) formation with an IC50 of 2.5 nM in LoVo cells to hydrogen peroxide (H2O2) to induce PAR synthesis.
Talazoparib (BMN-673) shows no effect on PARG activity as well as a protein panel.
Talazoparib (BMN-673) selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects。
Talazoparib (BMN-673) elicited remarkable antitumor activity in vivo xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency。

物理化学性质&存储条件

分子量 380.36
分子式 C19H14F2N6O
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

(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one

参考文献

1. Smith MA, et al. Clin Cancer Res. 2015 Feb 15;21(4):819-32.

2. Shen Y, et al. Clin Cancer Res. 2013 Sep 15;19(18):5003-15.

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