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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-PP-048
PP-048

Chemical Structure : PP-048

CAS No.:

PP-048 (PP048)

货号: PC-28106Not For Human Use, Lab Use Only.

PP-048 is a potent, selective, second-generation dual inhibitor of Polθ and PARP1 with IC50 of 4.9 nM and 6.8 nM, respectively, shows >226-fold selectivity over PARP2, PARP3, PARP5a/b, and PARP7.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PP-048 is a potent, selective, second-generation dual inhibitor of Polθ and PARP1 with IC50 of 4.9 nM and 6.8 nM, respectively, shows >226-fold selectivity over PARP2, PARP3, PARP5a/b, and PARP7.
PP-048 (10 mg/kg) achieved marked tumor growth inhibition (TGI = 91%) without eliciting the hematologic toxicity in MDA-MB-436 xenograft model.

物理化学性质&存储条件

分子量 733.25
分子式 C37H33ClN10O3S
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

2'-chloro-N-(5-((5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridin-2-yl)ethynyl)-1,3,4-thiadiazol-2-yl)-5'-methoxy-6-methyl-[4,4'-bipyridine]-3-carboxamide

参考文献

1. Ma L, et al. J Med Chem. 2026 Sep 10;69(17):20651-20677.

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