SU 9516
货号：
14796-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 14796-1mg |
| 描述 | SU 9516 is a 3-substituted indolinone that has anti-proliferative and pro-apoptotic activity in tumor cells. It is a potent inhibitor of several cyclin-dependent kinases (CDKs) with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1).1 It does not inhibit PKC, p38, PDGFR, or EGFR (IC50s = >10 µM).1 SU 9516 inhibits phosphorylation of the retinoblastoma protein pRb, resulting in increased pRb/E2F complex formation, cell-cycle arrest, and subsequent apoptosis.1,2 In leukemia cells (U937, Jurkat, and HL-60 cells) SU 9516 downregulates transcription of the antiapoptotic protein Mcl-1, leading to mitochondrial injury and cell death.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Lane, M.E.,Yu, B.,Rice, A., et al. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Research 61(16), 6170-6177 (2001).
2.Yu, B.,Lane, M.E. and Wadler, S. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochemical Pharmacology 64(7), 1091-1100 (2002).
3.Gao, N.,Kramer, L.,Rahmani, M., et al. The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism. Molecular Pharmacology 70(2), 645-655 (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 | 241.3 |
| 分子式 | C13H11N3O2 |
| CAS号 | 377090-84-1 |
| 稳定性 | ≥ 2 years |
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