中文名称: | Kobe0065 | ||||
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英文名称: | Kobe0065 | ||||
别名: | Kobe0065 N-(3-chloro-4-methylphenyl)-2-(2,6-dinitro-4-(trifluoromethyl)phenyl)hydrazinecarbothioamide | ||||
CAS No: | 436133-68-5 | 分子式: | C15H11ClF3N5O4S | 分子量: | 449.79 |
CAS No: | 436133-68-5 | ||||
分子式: | C15H11ClF3N5O4S | ||||
分子量: | 449.79 |
基本信息
产品编号: |
K10056 |
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产品名称: |
Kobe0065 |
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CAS: |
436133-68-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
449.79 |
-20℃ |
1个月 |
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化学名: |
N-(3-chloro-4-methylphenyl)-2-(2,6-dinitro-4-(trifluoromethyl)phenyl)hydrazinecarbothioamide |
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Solubility (25°C): |
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体外:
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DMSO |
89mg/mL (197.87mM) |
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Ethanol |
13mg/mL (28.9mM) |
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Water |
Insoluble |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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: |
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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: |
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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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )