2014年8月22日星期五

A-966492|cas 934162-61-5| DC Chem|Supplier|Price|Buy 

A-966492|cas 934162-61-5| DC Chem|Supplier|Price|Buy

DC Chemicals Supply: A-966492|cas 934162-61-5,Purity: >98% ,Cat No. DC7046, In stock.

Contact: website: www.dcchemicals.com,
sales@dcchemicals.com,order@dcchemicals.com,info@dcchemicals.com,
Tel: +86-21-61454686;Fax:+86-21-61642515;

A-966492|cas 934162-61-5 ,Synonym:  ,Chemical name: 2-(2-fluoro-4-((S)-pyrrolidin-2-yl)phenyl)-3H-benzo[d]imidazole-4-carboxamide ,Molecular Formula: C18H17FN4O ,MW:324.35

A-966492, cas 934162-61-5,Purity: >98%, Best Price and quality from DC Chemicals. A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

A-966492 is one of the most potent PARP inhibitors. A-966492 displays excellent potency against the PARP-1 enzyme with a Kiof 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. [1] A-966492 also demonstrates 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. In addition, A-966492 has excellent pharmaceutical properties and has demonstrated in vivo efficacy in preclinical mouse tumor models in combination with TMZ and carboplatin, as well as single agent activity in a BRCA1-deficient MX-1 tumor model. A-966492 is further characterized in Sprague?Dawley rats, beagle dogs, and cynomolgus monkeys, with A-966492 demonstrating oral bioavailabilities of 34?72% and half-lives of 1.7?1.9 hours. In vivo, A-966492 demonstrates significant enhancement of the efficacy of TMZ in a murine B16F10 syngeneic melanoma model, with the A-966492 combination groups showing superior efficacy. [1]

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