G-631 | TNKS inhibitor | Probechem Biochemicals

Chemical Structure : G-631

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G-631 (G631)

货号: PC-49499Not For Human Use, Lab Use Only.

G-631 is a potent and selective TNKS1/2 inhibitor with IC50 of 7 nM in biochemical assays of tankyrase auto-PARsylation activity, and cellular potency of 8 nM (HEK293).

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生物&药学活性

G-631 is a potent and selective TNKS1/2 inhibitor with IC50 of 7 nM in biochemical assays of tankyrase auto-PARsylation activity, and cellular potency of 8 nM (HEK293).
G-631 is selective against other PARP family members, with IC50 on PARP1 > 10,000 nM.
G-631 is also highly selective against kinases and secondary pharmacology targets, shows no >50 % inhibition against 220 kinases at 1 uM.
G-631 caused dose-dependent intestinal toxicity in mice while showing modest antitumor effects in a SW403 xenograft model at 100 mg/kg daily oral dosing.

物理化学性质&存储条件

分子量	420.42
分子式	C19H22F2N6O3
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	6-(4-(2,6-difluoro-4-(2-methoxyethoxy)phenyl)piperazin-1-yl)-1-methyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one

参考文献

1. Yu Zhong, et al. Toxicol Pathol. 2016 Feb;44(2):267-78.

G-631 (G631)

生物&药学活性

物理化学性质&存储条件

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G-631 (G631)

生物&药学活性

物理化学性质&存储条件

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