454453-49-7

中文名称 KOBE-2602

英文名称 kobe-2602

CAS 454453-49-7

分子式 C14H9F4N5O4S

分子量 419.31

MOL 文件 454453-49-7.mol

更新日期 2024/07/03 16:58:40

454453-49-7 结构式

基本信息物理化学性质图谱信息 KOBE-2602价格(试剂级) 常见问题列表

基本信息

中文别名

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

英文别名

CS-1280
kobe2602
kobe 2602
kobe-2602
kobe2602, >96%
Kobe 2602, >=98%
KOBE 2602
KOBE-2602
2-[2,6-Dinitro-4-(trifluoroMethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioaMide
Hydrazinecarbothioamide, 2-[2,6-dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)-
kobe-2602 2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide

所属类别

生物化工：激动剂抑制剂

物理化学性质

沸点450.8±55.0 °C(Predicted)

密度1.691±0.06 g/cm3(Predicted)

储存条件-20°C储存

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)

形态固体

颜色Light yellow to brown

图谱信息

KOBE-2602(454453-49-7)核磁图(¹HNMR)

KOBE-2602价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2024/04/30	S6527	KOBE-2602 Kobe2602	454453-49-7	2mg	877.29元
2024/04/30	HY-15717	KOBE-2602 Kobe2602	454453-49-7	10mM * 1mLin DMSO	1155元
2024/04/30	HY-15717	KOBE-2602 Kobe2602	454453-49-7	250mg	3360元

常见问题列表

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。

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.