计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
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.
Form:Solid
IC50& Target:EZH2
规格
规格或纯度
≥98%
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
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
914.02
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 125 mg/mL (136.76 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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