中文名 | kobe2602 |
英文名 | 2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide |
别名 | H-RAS·GTP与C-RAF-1RBD结合抑制剂(KOBE2602) 2-[2,6-二硝基-4-(三氟甲基)苯基]-N-(4-氟苯基)肼基硫代甲酰胺 |
英文别名 | CS-1280 kobe2602 kobe-2602 KOBE-2602 kobe 2602 2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide 2-[2,6-Dinitro-4-(trifluoroMethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioaMide kobe-2602 2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide |
CAS | 454453-49-7 |
化学式 | C14H9F4N5O4S |
分子量 | 419.31 |
密度 | 1.691±0.06 g/cm3(Predicted) |
沸点 | 450.8±55.0 °C(Predicted) |
酸度系数 | 9.35±0.70(Predicted) |
存储条件 | 2-8℃ |
体外研究 | Kobe2602 (2-20 μM; 1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells. Kobe2602 has IC 50 value of approximately 10 μM for the cellular Ras-Raf-binding inhibition. Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras G12V . Kobe2602 inhibits Ras⋅GTP but not Ras⋅GDP. Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-rasG12V-transformed cells. Cell Proliferation Assay Cell Line: H-ras G12V -transformed NIH 3T3 cells Concentration: 20 μM 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: 2 μM, 20 μM Incubation Time: 1 hour Result: Effectively reduced the amount of c-Raf-1 associated with H-Ras G12V in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras. |
体内研究 | Kobe2602 (80 mg/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-ras G12V gene. Animal Model: Female athymic nude mice (6-8 wk old), with SW480 cells xenograft Dosage: 80 mg/kg Administration: Oral administration, five consecutive days per week, for 17 days Result: Caused inhibition of the tumor growth. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.385 ml | 11.924 ml | 23.849 ml |
5 mM | 0.477 ml | 2.385 ml | 4.77 ml |
10 mM | 0.238 ml | 1.192 ml | 2.385 ml |
5 mM | 0.048 ml | 0.238 ml | 0.477 ml |
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