中文名称: | Kobe-2602 | ||||
---|---|---|---|---|---|
英文名称: | Kobe-2602 | ||||
别名: | Kobe-2602 Kobe2602;2-(2,6-dinitro-4-(trifluoromethyl)phenyl)-N-(4-fluorophenyl)hydrazinecarbothioamide | ||||
CAS No: | 454453-49-7 | 分子式: | C14H9F4N5O4S | 分子量: | 419.31 |
CAS No: | 454453-49-7 | ||||
分子式: | C14H9F4N5O4S | ||||
分子量: | 419.31 |
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: |
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. |
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 )