KOBE-2602
|
|
|
- CAS号:
- 454453-49-7
- 英文名:
- kobe-2602
- 英文别名:
- CS-1280;Kos2602;kobe2602;kobe 2602;kobe-2602;kobe2602, >96%;Kobe 2602, >=98%;KOBE 2602; KOBE-2602;Kobe2602, 10 mM in DMSO;2-[2,6-Dinitro-4-(trifluoroMethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioaMide
- 中文名:
- KOBE-2602
- 中文别名:
- KOS2602,RAS抑制剂;化合物KOBE2602,10 MM DMSO 溶液;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)肼硫代羰酰胺;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
- CBNumber:
- CB72667510
- 分子式:
- C14H9F4N5O4S
- 分子量:
- 419.31
- MOL File:
- 454453-49-7.mol
|
|
|
KOBE-2602化学性质
-
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:
-
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
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。
| 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
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2025/02/08 | HY-15717 | KOBE-2602
Kobe2602 | 454453-49-7 | 5 mg | 251元 |
| 2025/02/08 | HY-15717 | KOBE-2602
Kobe2602 | 454453-49-7 | 10mM * 1mLin DMSO | 276元 |
454453-49-7, KOBE-2602 相关搜索:
- Aromatics, Miscellaneous Reagents, Pharmaceuticals, Intermediates & Fine Chemicals
- Inhibitors
- 抑制剂
- 药靶配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- C14H9F4N5O4S
- 化合物KOBE2602,10 MM DMSO 溶液
- 2-[2,6-二硝基-4-(三氟甲基)苯基]-N-(4-氟苯基)肼硫代羰酰胺
- KOS2602,RAS抑制剂
- 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
- 454453-49-7
- Kobe2602, 10 mM in DMSO
- Kos2602
- H-Ras,Inhibitor,antiproliferative,Kobe-2602,carcinoma,Kobe 2602,Kobe2602,inhibit,Ras,Raf
- Hydrazinecarbothioamide, 2-[2,6-dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)-
- KOBE 2602; KOBE-2602
- CS-1280
- kobe2602, >96%
- Kobe 2602, >=98%
- 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
- kobe2602
- kobe 2602