ZM 336372 is a potent inhibitor of human c-Raf, with an IC50 value of 0.07 μM in a standard assay containing 0.1 mM ATP. The IC50 value decreases to 0.01 μM at 0.025 mM ATP and increases to 0.9 μM at 2.5 mM ATP, indicating that ZM 336372 competitively inhibits with respect to ATP. Additionally, ZM 336372 is ten times more effective in inhibiting c-Raf compared to B-Raf[1]. Cell proliferation analysis using ZM336372 was conducted with the 3,4-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide growth assay on H727 and BON cells treated with control (DMSO) and 100 μM ZM336372 for up to 16 and 10 days, respectively. Both H727 and BON cell proliferation were inhibited in the presence of the drug compared to the controls. Specifically, H727 cells exhibited suppressed growth with ZM336372 treatment, with significantly less growth observed by day 6, continuing through day 16. Similarly, BON cells showed growth suppression starting from day 4, which persisted until day 10[2].
体外研究
ZM 336372 is a potent inhibitor of human c-Raf, with an IC50 value of 0.07 μM in a standard assay containing 0.1 mM ATP. The IC50 value decreases to 0.01 μM at 0.025 mM ATP and increases to 0.9 μM at 2.5 mM ATP, indicating that ZM 336372 competitively inhibits with respect to ATP. Additionally, ZM 336372 is ten times more effective in inhibiting c-Raf compared to B-Raf[1].
Cell proliferation analysis using ZM336372 was conducted with the 3,4-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide growth assay on H727 and BON cells treated with control (DMSO) and 100 μM ZM336372 for up to 16 and 10 days, respectively. Both H727 and BON cell proliferation were inhibited in the presence of the drug compared to the controls. Specifically, H727 cells exhibited suppressed growth with ZM336372 treatment, with significantly less growth observed by day 6, continuing through day 16. Similarly, BON cells showed growth suppression starting from day 4, which persisted until day 10[2].
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