KOBE-2602
- CAS号:454453-49-7
- 英文名:kobe-2602
- 中文名:KOBE-2602
- CBNumber:CB72667510
- 分子式:C14H9F4N5O4S
- 分子量:419.31
- MOL File:454453-49-7.mol
- 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 :insoluble in H2O; ≥17 mg/mL in DMSO; ≥17.53 mg/mL in EtOH with ultrasonic
- 酸度系数(pKa) :9.35±0.70(Predicted)
- 形态 :solid
- 颜色 :Light yellow to brown
KOBE-2602性质、用途与生产工艺
- 生物活性 Kobe2602是选择性Ras抑制剂，抑制H-Ras GTP与c-Raf-1结合，Ki值为149 μM。
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靶点
Target Value Ras
()149 μM(Ki) -
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.
- 更新日期：2024/11/08
- 产品编号：HY-15717
- 产品名称：KOBE-2602 Kobe2602
- CAS编号：454453-49-7
- 包装：50mg
- 价格：1050元
- 更新日期：2024/11/08
- 产品编号：HY-15717
- 产品名称：KOBE-2602 Kobe2602
- CAS编号：454453-49-7
- 包装：10mM * 1mLin DMSO
- 价格：1155元
- 公司名称：TORONTO
- 联系电话：--
- 电子邮件：info@trc-canada.com
- 国家：加拿大
- 产品数：6038
- 优势度：71
