产品
编 号：F750126
分子式：C56H71N7O9S
分子量：1018.27
分子式：C56H71N7O9S
分子量：1018.27
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CAS No: 2230914-84-6
产品详情
生物活性：
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma.
体内研究：
YM281 (80, 100 mg/kg; i.v.; 6 times for 3 weeks) shows antitumor effects and significantly reduces the expression of EZH2 protein and H3K27me3 levels.Animal Model:Balb/c nude mice (SU-DHL-6 xenograft model)
Dosage:80 mg/kg
Administration:I.v.; 6 times for 3 weeks
Result:Remarkably suppressed the tumor volume and significantly reduced the EZH2 protein and H3K27me3 levels.
Animal Model:Balb/c nude mice (Jeko-1 xenograft model)
Dosage:100 mg/kg
Administration:I.v.; 6 times for 3 weeks
Result:Shows anti-tumor effects with the significantly reduced the expression of EZH2 protein and H3K27me3 levels.
体外研究：
YM281 (compound V2) (0-6 μM; 0-48 h) decreases the EZH2 protein level and the PRC2 (polycomb repressive complex 2) complex through the VHL (vonHippel?Lindau)-dependent ubiquitin-proteasome system.YM281 (0-10 μM; 24 h) shows anticancer effects in lymphoma cells.YM281 (0-5 μM) induces cell apoptosis and cell cycle arrest at the G0/G1 phase.YM281 (0-5 μM; 24 h) increases the activity of caspase-3 and -7 and meanwhile reduces the cell viability in primary lymphoma cells.
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma.
体内研究：
YM281 (80, 100 mg/kg; i.v.; 6 times for 3 weeks) shows antitumor effects and significantly reduces the expression of EZH2 protein and H3K27me3 levels.Animal Model:Balb/c nude mice (SU-DHL-6 xenograft model)
Dosage:80 mg/kg
Administration:I.v.; 6 times for 3 weeks
Result:Remarkably suppressed the tumor volume and significantly reduced the EZH2 protein and H3K27me3 levels.
Animal Model:Balb/c nude mice (Jeko-1 xenograft model)
Dosage:100 mg/kg
Administration:I.v.; 6 times for 3 weeks
Result:Shows anti-tumor effects with the significantly reduced the expression of EZH2 protein and H3K27me3 levels.
体外研究：
YM281 (compound V2) (0-6 μM; 0-48 h) decreases the EZH2 protein level and the PRC2 (polycomb repressive complex 2) complex through the VHL (vonHippel?Lindau)-dependent ubiquitin-proteasome system.YM281 (0-10 μM; 24 h) shows anticancer effects in lymphoma cells.YM281 (0-5 μM) induces cell apoptosis and cell cycle arrest at the G0/G1 phase.YM281 (0-5 μM; 24 h) increases the activity of caspase-3 and -7 and meanwhile reduces the cell viability in primary lymphoma cells.
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