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Kobe0065  ≥98%(HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(≥40mg/mL)
产品描述：基本信息 产品编号： K10056  产品名称： Kobe0065 CAS: 436133-68-5   储存条件 粉末 -20℃ 四年     分子式： C15H11ClF3N5O4S 溶于液体 -80℃ 6个月 分子量： 449.79 -20℃ 1个月 化学名：  N-(3-chloro-4-methylphenyl)-2-(2,6-dinitro-4-(trifluoromethyl)phenyl)hydrazinecarbothioamide Solubility (25°C)：   体外:   DMSO 89mg/mL (197.87mM) Ethanol 13mg/mL (28.9mM) 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 2.2233mL 11.1163mL 22.2326mL 5mM 0.4447mL 2.2233mL 4.4465mL 10mM 0.2223mL 1.1116mL 2.2233mL 50mM 0.0445mL 0.2223mL 0.4447mL   生物活性 产品描述 一种新型的有效的Ras-Raf相互作用抑制剂，能够完全抑制H-Ras·GTP与c-Raf-1 RBD的结合，Ki值：46±13μM。 靶点 H-Ras   体外研究 Kobe0065-family compounds bind to Ras•GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes.The compounds efficiently inhibit the interaction of Ras•GTP with their multiple effectors including Raf,PI3K,and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases,which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition.The phosphorylation of downstream kinases MEK and ERK is effectively attenuated by 20μM Kobe0065 and Kobe2602 in NIH3T3 cells transiently expressing H-RasG12V. 体内研究 Kobe0065 and Kobe2602 exhibit antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the Kras(G12V) gene by oral administration.   推荐实验方法(仅供参考) 细胞实验:   Cells (2×103) are seeded in a 96-well plate and cultured in DMEM containing 2% (vol/vol) FBS in the presence of one of the compounds.Viable cell numbers are measured by formazan formation using a Cell Counting Kit 8.Apoptotic cells are detected by a standard TUNEL assay using an In Situ Cell Detection kit.   动物实验:   Cells (5×106) are implanted into the right flanks of female athymic nude mice (6-8 wk old).After tumor sizes reached appr 50mm3 on average,compounds suspended in Cremophor:ethanol:water (1:1:6) are administered orally for five consecutive days per week for 17 d.Tumor volumes (V) are calculated.Dissected tumors after 17-d administration of the 80mg/kg compounds are fixed in 4% (wt/vol) paraformaldehyde and embedded in paraffin.Their sections are subjected to immunohistochemistry with an anti-ERK1/2 antibody or an anti-CD31 antibody using a HISTMOUSE-PLUS kit.Apoptotic cells are detected by a TUNEL assay.Statistical significance for groups of three or more is determined by one-way ANOVA with Tukey’s test for post hoc analysis.
保存条件：-20℃

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