计算溶液所需的质量、体积或浓度。
概述
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 IC 50 ): 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
In Vitro
MS177 inhibits the enzymatic activities of EZH2-PRC2 (IC 50 : 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 IC 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: AML cell line: MV4;11, MOML-13, RS4;11, KOPN-8 THP-1, EOL-1 (MLL-r cells) Control cell line: K562 (CML cells) Patient sample: AML cells Concentration: 0-100 μM approximately Incubation Time: 4 days Result: Inhibited cell proliferation with IC 50 s of 0.1-0.57 μM for MLL-r cells, 0.09-1.35 μM for Patient sample, >100 μM for K562 cell. Western Blot AnalysisCell Line: EOL-1 cell Concentration: 0.1, 0.5, 1, 2.5, 5 μM Incubation Time: 16 h Result: Depleted EZH2, EED and SUZ12 in a concentration-dependent manner and suppressed global H3K27me3.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
IC50& Target:EZH2
规格
规格或纯度
10mM in DMSO
英文名称
MS177
生化机理
MS177 是一种高效、速效的 EZH2 降解剂。MS177 是一种 PROTAC，由 CRBN 配体、连接体和强效酶 EZH2 抑制剂 C24（C24 IC 50 ）组成：12u2009nM）。MS177 可有效地消耗规范 EZH2-PRC2 和非规范 EZH2-cM
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
分子量
914.02
高级数据
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2225938-86-1，分子式为 C48H55N11O8，分子量为 914.02 g/mol。
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