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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.
CAS Number: 934162-61-5
Description: A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
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.
Target: PARP1,PARP2
Biosafety Level: Not applicable (BSL-1)
References: Penning TD, et al. J Med Chem. 2010 Apr 22;53(8):3142-53.
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