JNJ-7706621
货号：
18494-1mg 基本售价：
490.0 元 规格：
1 mg
产品信息
概述| 货号 | 18494-1mg |
| 描述 | JNJ-7706621 is a dual inhibitor of cyclin-dependent kinases (CDKs) and Aurora kinases. It potently inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk3/cyclin E, Cdk4/cyclin D1, Cdk6/cyclin D1, Aurora A, and Aurora B in vitro(IC50s = 9, 4, 3, 58, 253, 175, 11, and 15 nM, respectively).1 It shows selectivity for these enzymes over a panel of other receptors and kinases, although it exhibits submicromolar inhibition of VEGF and FGF receptors, as well as GSK3β.1 JNJ-7706621 blocks the growth of a large variety of cancer cell lines (IC50 values range from 112 to 514 nM), with lower potency against normal cells (IC50 values between 3.67 and 5.42 µM). It induces the regression of A375 melanoma human tumor xenografts in mice.1 JNJ-7706621 is a substrate for the ATP-binding cassette transporter G2, also known as breast cancer resistance protein.2 |
| 别名 | Aurora A Inhibitor I;Aurora Kinase/CDK Inhibitor; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Emanuel, S.,Rugg, C.A.,Gruninger, R.H., et al. The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Cancer Research 65(19), 9038-9046 (2005).
2.Seamon, J.A.,Rugg, C.A.,Emanuel, S., et al. Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor. Molecular Cancer Therapeutics 5(10), 2459-2467 (2006).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 394.4 |
| 分子式 | C15H12F2N6O3S |
| CAS号 | 443797-96-4 |
| 稳定性 | ≥ 2 years |
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