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Chemical Structure : G-631
Catalog No.: 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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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.
| M.Wt | 420.42 | |
| Formula | C19H22F2N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Yu Zhong, et al. Toxicol Pathol. 2016 Feb;44(2):267-78.
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