KOBE-2602
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 |
KOBE-2602 用途与合成方法
| 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. |
KOBE-2602 价格(试剂级)
| 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 | 454453-49-7 | 50mg | 1050 |
| 2024-11-08 | HY-15717 | KOBE-2602 | 454453-49-7 | 10mM * 1mLin DMSO | 1155 |
