kobe 2602
2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide
CAS: 454453-49-7
Molecular Formula: C14H9F4N5O4S
kobe 2602 - Names and Identifiers
kobe 2602 - Physico-chemical Properties
| Molecular Formula | C14H9F4N5O4S |
| Molar Mass | 419.31 |
| Density | 1.691±0.06 g/cm3(Predicted) |
| Boling Point | 450.8±55.0 °C(Predicted) |
| pKa | 9.35±0.70(Predicted) |
| Storage Condition | 2-8℃ |
| In vitro study | 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. |
| In vivo study | 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. |
kobe 2602 - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
kobe 2602 - Reference Information
| biological activity | Kobe2602 is a selective Ras inhibitor, inhibiting the binding of H-Ras GTP to c-Raf-1 with a Ki value of 149 μM. |
| target | TargetValue Ras () 149 μ m (Ki) |
| Target | Value |
| Ras () | 149 μM(Ki) |
| in vitro study | Kobe2602 (2-20μM; 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 RasGTP but not RasGDP. Kobe2602 (20 μ M) inhibits the anchorage-dependent proliferation of H-rasG12V-transformed cells. Cell Proliferation Assay Cell Line: H-ras G12V-transformed NIH 3T3 cells Concentration: 20 μ M 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 μ M, 20 μ M 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. |
| Cell Line: | H-ras G12V -transformed NIH 3T3 cells NIH 3T3 cells |
| Concentration: | 20 μM 2 μM, 20 μM |
| Incubation Time: | 24 hours , 48 hours, 72 hours 1 hour |
| Result: | Efficiently inhibited colony formation in soft agar in a dose-dependent manner. 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. Caused inhibition of the tumor growth. |
| in vivo study | 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: used inhibition of the tumor growth. |
| 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 |
Last Update：2024-04-09 20:52:54
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Tel: 609-228-6898
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