A-966492
Catalog #
27601-1
$175
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Description
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
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Synonyms
2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide
Product Info
Storage and Usage
Citations
Purity
≥98% by HPLC
Target(s)
PARP1,PARP2
Formula
C18H17FN4O
MW
324.4 Da
Solubility
Soluble in DMSO 65 mg/ml,Water <1 mg/ml,Ethanol <1 mg/ml
CAS Registry #
934162-61-5
Background
A-966492 is one of the most potent PARP inhibitors. A-966492 displays excellent potency against the PARP-1 enzyme with a Ki of 1 nM and an EC50 of 1 nM in a whole cell assay. A-966492 significantly enhances the efficacy of TMZ in a dose-dependent manner. In addition, A-966492 is orally bioavailable across multiple species, crosses the blood?brain barrier, and appears to distribute into tumor tissue. A-966492 represents a promising, structurally diverse benzimidazole analogue and is being further characterized preclinically.
References
Penning TD, et al. J Med Chem. 2010 Apr 22;53(8):3142-53.
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