CEP-32496
货号：
18776-500ug 基本售价：
490.0 元 规格：
500 ug
产品信息
概述| 货号 | 18776-500ug |
| 描述 | B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.1 Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.1 CEP-32496 is a potent inhibitor of B-RafV600E(Kd = 14 nM in an in vitro binding assay).2 It blocks B-RafV600E-dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC50s = 78 and 60 nM, respectively).2 CEP-32496 binds kinases other than B-Raf but displays selective cytotoxicity for cells expressing B-RafV600E.2 It displays good oral bioavailability in rats, dogs, and monkeys and has single oral dose pharmacodynamics inhibition of both pMEK and pERK in B-RafV600E colon carcinoma xenografts in nude mice.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Tronnier, M., and Mitteldorf, C. Treating advanced melanoma: Current insights and opportunities. Cancer Manag.Res. 6, 349-356 (2014).
2.James, J.,Ruggeri, B.,Armstrong, R.C., et al. CEP-32496: a novel orally active BRAFV600E inhibitor with selective cellular and in vivo antitumor activity. Molecular Cancer Therapeutics 11(4), 930-941 (2012).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 517.5 |
| 分子式 | C24H22F3N5O5 |
| CAS号 | 1188910-76-0 |
| 稳定性 | ≥ 2 years |
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