A-966492

Catalog #: 27601-1
Size: 5 mg
$170
MW: 324.4 Da
CAS Registry #: 934162-61-5
Formula: C18H17FN4O
Target: PARP1,PARP2
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.
Description:
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
Synonym(s):
2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide
Purity:

≥98% by HPLC

Solubility:
Soluble in DMSO 65 mg/ml,Water <1 mg/ml,Ethanol <1 mg/ml
Storage / Stability:

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

Reference(s):
Penning TD, et al. J Med Chem. 2010 Apr 22;53(8):3142-53.
Scientific Category:
PARP Inhibitor
Product Type:
Inhibitor
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