Kobe2602 is an effective small-molecule compound inhibiting Ras–Raf interaction by SBDD exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 149 ± 55 μM.
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Kobe2602 is an inhibitor of the Ras-Raf interaction, preventing the binding of H-Ras·GTP to the c-Raf-1 RBD with a Ki of 149 μM and demonstrating antitumor activity[1].
体内研究
Administered orally at 80 mg/kg for five consecutive days each week over 17 days, Kobe2602 displays antitumor activity against a xenograft model of human colon carcinoma SW480 cells with the K-RasG12V mutation[1].
体外研究
At concentrations ranging from 2 to 20 μM over one hour, Kobe2602 inhibits Ras-Raf binding in NIH 3T3 cells with an IC50 of approximately 10 μM[1].
At 20 μM, it effectively suppresses the phosphorylation of downstream kinases MEK and ERK in NIH 3T3 cells expressing H-RasG12V and inhibits the anchorage-dependent proliferation of cells transformed by H-RasG12V[1].
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