Kobe-2602  ≥98%(HPLC)

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包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(12mg/mL 超声 加热)
产品描述:基本信息 产品编号: K10059 产品名称: Kobe-2602 CAS: 454453-49-7   储存条件 粉末 -20℃ 四年     分子式: C14H9F4N5O4S 溶于液体 -80℃ 6个月 分子量: 419.31 -20℃ 1个月 化学名:  2-(2,6-dinitro-4-(trifluoromethyl)phenyl)-N-(4-fluorophenyl)hydrazinecarbothioamide Solubility (25°C):   体外:   DMSO 84mg/mL (200.32mM) Ethanol 40mg/mL (95.39mM) Water Insoluble 体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3849mL 11.9244mL 23.8487mL 5mM 0.4770mL 2.3849mL 4.7697mL 10mM 0.2385mL 1.1924mL 2.3849mL 50mM 0.0477mL 0.2385mL 0.4770mL   生物活性 产品描述 一种高效、选择性的RAS抑制剂,对H-RAS-GTP-c-Raf-1具有体内外结合的抑制活性。 靶点 Ras  149 μM(Ki)   体外研究 Kobe2602 (2-20μM;1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells.Kobe2602 has IC50 value of approximately 10μM for the cellular Ras-Raf-binding inhibition.Kobe2602 (20μM) efficiently inhibits the phosphorylation of MEK and ERK,downstream kinases of Raf in NIH 3T3 cells transiently expressing H-RasG12V.Kobe2602 inhibits RasGTP but not RasGDP.Kobe2602 (20μM) inhibits the anchorage-dependent proliferation of H-RasG12V-transformed cells. Cell Proliferation Ass Cell Line: H-rasG12V-transformed NIH 3T3 cells Concentration: 20μM Incubation Time: 24 hours,48 hours,72 hours Result: Efficiently inhibited colony formation in soft agar in a dose-dependent manner. Western Blot Analysis Cell Line: NIH 3T3 cells Concentration: 2μM,20μM Incubation Time: 1 hours Result: Effectively reduced the amount of c-Raf-1 associated with H-RasG12V in NIH 3T3 cells in a dose-dependent manner,indicating the inhibition of the cellular activity of Ras. 体内研究 Kobe2602 (80mg/kg;p.o.;five consecutive days per week;for 17 days) exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-RasG12V gene. Animal Model: Female athymic nude mice (6-8 wk old),with SW480 cells xenograft Dosage: 80mg/kg Administration: Oral administration, five consecutive days per week,for 17 days Result: Caused inhibition of the tumor growt.
保存条件:-20℃