Simmiparib |CAS:1551355-46-4 Probechem Biochemicals

Chemical Structure : Simmiparib

CAS No.: 1551355-46-4

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Simmiparib

货号: PC-61950Not For Human Use, Lab Use Only.

Simmiparib is a novel potent, orally active PARP1/2 inhibitor with IC50 of 1.75/0.22 nM, inhibits PARP1 >90-fold more potently than the other PARPs (PARP3, TNKS1, TNKS2).

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生物&药学活性

Simmiparib is a novel potent, orally active PARP1/2 inhibitor with IC50 of 1.75/0.22 nM, inhibits PARP1 >90-fold more potently than the other PARPs (PARP3, TNKS1, TNKS2).
Simmiparib selectively induces the accumulation of DNA double-strand breaks, G2/M arrest and apoptosis in homologous recombination repair (HR)-deficient cells.
Simmiparib potentiates the proliferative inhibition of several conventional anticancer drugs, reduces the poly(ADP-ribose) formation in HR-deficient cancer cells and xenografts.
Simmiparib exhibits 10-fold greater growth inhibition than olaparib against HR-deficient human cancer cell- or tissue-derived xenografts in nude mice.

物理化学性质&存储条件

分子量	486.431
分子式	C23H18F4N6O2
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	4-(4-fluoro-3-(5-methyl-3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)benzyl)phthalazin-1(2H)-one

参考文献

1. Yuan B, et al. Cancer Lett. 2017 Feb 1;386:47-56.

2. Yang ZM, et al. Acta Pharmacol Sin. 2017 Jul;38(7):1038-1047.

Simmiparib

生物&药学活性

物理化学性质&存储条件

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Simmiparib

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物理化学性质&存储条件

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