KOBE-2602
| 中文名称 | KOBE-2602 |
|---|---|
| 中文同义词 | 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;H-RAS·GTP与C-RAF-1RBD结合抑制剂(KOBE2602);KOS2602,RAS抑制剂;2-[2,6-二硝基-4-(三氟甲基)苯基]-N-(4-氟苯基)肼硫代羰酰胺 |
| 英文名称 | kobe-2602 |
| 英文同义词 | kobe 2602;kobe2602;kobe-2602;2-[2,6-Dinitro-4-(trifluoroMethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioaMide;kobe-2602 2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide;Kobe 2602, >=98%;kobe2602, >96%;CS-1280 |
| CAS号 | 454453-49-7 |
| 分子式 | C14H9F4N5O4S |
| 分子量 | 419.31 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors;Aromatics, Miscellaneous Reagents, Pharmaceuticals, Intermediates & Fine Chemicals |
| Mol文件 | 454453-49-7.mol |
| 结构式 |  |
KOBE-2602 性质
| 沸点 | 450.8±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.691±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 不溶于水； DMSO 中≥17 mg/mL； ≥17.53 mg/mL，乙醇溶液，超声波 |
| 酸度系数(pKa) | 9.35±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至棕色 |
| Target | Value |
|
Ras
() | 149 μM(Ki) |
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. |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-15717 | KOBE-2602 Kobe2602 | 454453-49-7 | 50mg | 1050元 |
| 2024/11/08 | HY-15717 | KOBE-2602 Kobe2602 | 454453-49-7 | 10mM * 1mLin DMSO | 1155元 |