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454453-49-7

中文名稱 KOBE-2602
英文名稱 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 2024/12/23 09:08:07
454453-49-7 結(jié)構(gòu)式 454453-49-7 結(jié)構(gòu)式

基本信息

中文別名
H-RAS·GTP與C-RAF-1RBD結(jié)合抑制劑(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
英文別名
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

沸點450.8±55.0 °C(Predicted)
密度1.691±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度insoluble in H2O; ≥17 mg/mL in DMSO; ≥17.53 mg/mL in EtOH with ultrasonic
酸度系數(shù)(pKa)9.35±0.70(Predicted)
形態(tài)固體
顏色Light yellow to brown
KOBE-2602價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-15717KOBE-2602
Kobe2602
454453-49-750mg1050元
2024/11/08HY-15717KOBE-2602
Kobe2602
454453-49-710mM * 1mLin DMSO1155元
2024/11/08HY-15717KOBE-2602
Kobe2602
454453-49-7100mg1680元

常見問題列表

生物活性
Kobe2602是選擇性Ras抑制劑,抑制H-Ras GTP與c-Raf-1結(jié)合,Ki值為149 μM。
靶點
TargetValue
Ras
()
149 μM(Ki)
體外研究

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.
體內(nèi)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.
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