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Apexbio Technology LLC A-966492 934162-61-5 50mg

Supplier: Apexbio Technology LLC A416050
A-966492 (CAS 934162-61-5) is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) exhibiting a Ki of 1 nM It also inhibits PARP-2 with a Ki of approximately 1 5 nM As a PARP inhibitor this compound interferes with the enzymatic activity essential for DNA repair pathways sensitizing cancer cells to cytotoxic therapies In vitro A-966492 shows effective inhibition in C41 cells with an EC50 of 1 nM and demonstrates moderate oral bioavailability (34-72%) and a half-life of around 1 7-1 9 hours It crosses the blood-brain barrier and has demonstrated activity in preclinical murine cancer models including B16F10 melanoma and BRCA1-deficient MX-1 breast cancer xenografts enhancing the efficacy of chemotherapeutic agents such as temozolomide and carboplatin
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