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- 2025年07月15日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
934162-61-5
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1377.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥480.0 |
| 规格： | 5 mg | 产品价格： | ￥1252.0 |
| 规格： | 10 mg | 产品价格： | ￥2280.0 |
| 规格： | 50 mg | 产品价格： | ￥7080.0 |
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A-966492
CAS No. : 934162-61-5
MCE 国际站：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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