Kobe 0065
货号:
16261-1mg 基本售价:
406.0 元 规格:
1 mg
产品信息
概述货号 | 16261-1mg |
描述 | The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 0065 is an orally active Ras inhibitor with selectivity for H-Ras (Ki = 46 μM).1 It can inhibit both anchorage-dependent and -independent growth and induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = ~1.5 μM), which leads to a down-regulation of MEK/ERK, Akt, RalA, and Son of sevenless.1 At an oral dose of 80 mg/kg, Kobe 0065 also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.1 |
性能供应商 | Cayman |
应用文献 |
1.Shima, F.,Yoshikawak, Y.,Ye, M., et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proceedings of the National Academy of Sciences of the United States of America 110(20), 8182-8187 (2013).
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运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 449.8 |
分子式 | C15H11ClF3N5O4S |
CAS号 | 436133-68-5 |
稳定性 | ≥ 2 years |
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