产品
编 号：F762411
分子式：C48H55N11O8
分子量：914.02
分子式：C48H55N11O8
分子量：914.02
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2225938-86-1
产品详情
生物活性：
MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12?nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
体内研究：
MS177 (100?mg/kg, i.p., BID for 6 days) represses tumor growth in PDX animal model of MLL-r AML, and in subcutaneously xenografted MLL-r leukaemia models.MS177 (50 mg/kg, i.p.) achieves intraplasma concentrations about 1 μM in male Swiss Albino mice.MS177 (100?mg/kg, i.p., BID for 6?days per week; and 200?mg/?kg, i.p. BID 3?days per week) is well tolerated and lacks apparent toxicity in mice.Animal Model:PDX animal model of MLL-r AML
Dosage:100?mg/kg
Administration:Intraperitoneal injection (i.p.), BID for 6 days.
Result:Inhibited tumor growth and prolonged survival.
体外研究：
MS177 inhibits the enzymatic activities of EZH2-PRC2 (IC50: 7?nM).MS177 (5 μM, 24 h) decreases H3K27me3 and increases H3K27activity in HeLa cells.MS177 (0.1-5 μM, 16 h) effectively degrades cellular EZH2-PRC2 and suppresses global H3K27me3 in EOL-1 cells.MS177 (0.1-5 μM, 16 h) induces Myc degradation in EOL-1 and MV4 cells.MS177 (4 days) shows antiproliferation effects in a panel of MLL-r leukaemia cells and samples from patients with AML, with IC50s below 2 μM.MS177 (0.5-2.5 μM, 24 h) decreases colony-forming capabilities in MV4;11 cells.MS177 (0.5-2.5 μM, 24 h) slows cell cycle progression and induces MOLM-13 cell apoptosis.
MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12?nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
体内研究：
MS177 (100?mg/kg, i.p., BID for 6 days) represses tumor growth in PDX animal model of MLL-r AML, and in subcutaneously xenografted MLL-r leukaemia models.MS177 (50 mg/kg, i.p.) achieves intraplasma concentrations about 1 μM in male Swiss Albino mice.MS177 (100?mg/kg, i.p., BID for 6?days per week; and 200?mg/?kg, i.p. BID 3?days per week) is well tolerated and lacks apparent toxicity in mice.Animal Model:PDX animal model of MLL-r AML
Dosage:100?mg/kg
Administration:Intraperitoneal injection (i.p.), BID for 6 days.
Result:Inhibited tumor growth and prolonged survival.
体外研究：
MS177 inhibits the enzymatic activities of EZH2-PRC2 (IC50: 7?nM).MS177 (5 μM, 24 h) decreases H3K27me3 and increases H3K27activity in HeLa cells.MS177 (0.1-5 μM, 16 h) effectively degrades cellular EZH2-PRC2 and suppresses global H3K27me3 in EOL-1 cells.MS177 (0.1-5 μM, 16 h) induces Myc degradation in EOL-1 and MV4 cells.MS177 (4 days) shows antiproliferation effects in a panel of MLL-r leukaemia cells and samples from patients with AML, with IC50s below 2 μM.MS177 (0.5-2.5 μM, 24 h) decreases colony-forming capabilities in MV4;11 cells.MS177 (0.5-2.5 μM, 24 h) slows cell cycle progression and induces MOLM-13 cell apoptosis.
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