Brief Description

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
IC50 value: 1 nM/1.5 nM (Ki, PARP1/PARP2)
Target: PARP inhibitor
A-966492 displayed excellent potency against the PARP-1 enzyme with a K(i) of 1 nM and an EC(50) of 1 nM in a whole cell assay. A-966492 is orally bioavailable across multiple species, crosses the blood-brain barrier, and appears to distribute into tumor tissue. A-966492 also demonstrated 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.

Solubility

DMSO > 60 mg/ml

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White to off-white solid