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A-966492
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A-966492
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.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | XAV-939 | Rucaparib | PJ34 | 3-Aminobenzamide | G007-LK | Dehydrocorydaline chloride | AG14361 | Iniparib | AZD-2461 | BGP-15 | Fucosterol | JW 55 | EB-47 dihydrochloride | UPF 1069 | AZ6102 | iRucaparib-AP6 | ME0328 | MN-64 | 5,?7,?4'-?Trimethoxyflavone | Benzamide | GeA-69 | Paris saponin VII | PARP14 inhibitor H10 | BYK204165 | NU1025 | Oroxin A
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