Description
As a novel inhibitor, A-966492 can potently inhibit PARP1 and PARP2 with Ki of 1 nM and 1.5 nM,
Storage
2 years at -20 centigrade
Molecular Formula
C18H17FN4O
Chemical Name
2-(2-fluoro-4-((S)-pyrrolidin-2-yl)phenyl)-3H-benzo[d]imidazole-4-carboxamide
Solubility
DSMO 65 mg/mL Water
In vitro
A-966492 is one of the most potent PARP inhibitors. A-966492 displays excellent potency against the PARP-1 enzyme with a Kiof 1 nM.
In vivo
A-966492 shows good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin. In vivo, A-966492 demonstrates significant enhancement of the efficacy of TMZ in a murine B16F10 syngeneic melanoma model, with the A-966492 combination groups showing superior efficacy.
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