型号:
产品价格:电议      采购度:1612      原产地:美洲
发布时间:2021/7/29 18:28:39 所属地区:上海 上海市
简要描述:
A-966492 是一种新颖的,有效的 PARP1 和 PARP2 抑制剂,Ki 值为 1 nM 和 nM。
标签:a-966492
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CAS No. : 934162-61-5
MCE 站:A-966492
产品活性:A-966492 是一种新颖的,有效的 PARP1 和 PARP2 抑制剂,Ki 值为 1 nM 和 1.5 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:PARP
In Vitro: 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.
In Vivo: A-966492 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.
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更新时间:2024/1/2 10:17:03
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