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

Chemical Structure : Pamiparib

CAS No.: 1446261-44-4

Pamiparib (BGB-290, BGB290)

货号: PC-60483Not For Human Use, Lab Use Only.

Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with IC50 of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with IC50 of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively.
Pamiparib (BGB-290) is high selectivity over other PARP enzymes.
Pamiparib (BGB-290) shows potent DNA-trapping activity with IC50 of 13 nM in vitro.
Pamiparib (BGB-290) potently inhibits intracellular PAR formation with an IC50 of 0.24 nM in cellular assays,  is highly active both in vitro and in vivo in BRCA mutant tumor cells.
Oral administration of BGB-290 resulted in time-dependent and dose-dependent inhibition of PARylation in MDA-MB-436 (BRCA1 mutant) breast cancer xenograft, over 10-fold more potent than olaparib.

物理化学性质&存储条件

分子量 298.32
分子式 C16H15FN4O
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

(10aR)-2-fluoro-10a-methyl-5,8,9,10,10a,11-hexahydro-5,6,7a,11- tetraazacyclohepta[def]cyclopenta[a]fluoren-4(7H)-one

参考文献

1. Zhiyu Tang, et al. Cancer Res (2015) 75 (15_Supplement): 1653.

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