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编 号:F361537
分子式:C14H9F4N5O4S
分子量:419.31
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10mM*1mL in DMSO
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50mg
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100mg
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250mg
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生物活性:
Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity.

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-RasG12V 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.

体外研究:
Kobe2602 (2-20 μM; 1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells.Kobe2602 has IC50 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-RasG12V.Kobe2602 inhibits Ras?GTP but not Ras?GDP.Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-RasG12V-transformed cells.
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