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MS177
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MS177图片
CAS NO:2225938-86-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
MS177 是一种有效且快速起效的EZH2降解剂。MS177 是一种PROTAC分子,由 CRBN 配体、连接子和有效的酶促 EZH2 抑制剂 C24 组成 (C24IC50: 12 nM)。MS177 可有效地消耗剥离 EZH2-PRC2 和非经典 EZH2-cMyc 复合物。MS177 抑制白血病细胞生长、诱导细胞凋亡和细胞周期阻滞。
生物活性

MS177 is an effective and fast-actingEZH2degrader. MS177 is aPROTACthat consists of a CRBN ligand, linker, and a potent enzymaticEZH2 inhibitorC24 (C24IC50): 12 nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition,apoptosisand cell cycle progression arrest[1].

IC50& Target[1]

EZH2

 

体外研究
(In Vitro)

MS177 inhibits the enzymatic activities of EZH2-PRC2 (IC50: 7 nM)[1].
MS177 (5 μM, 24 h) decreases H3K27me3 and increases H3K27activity in HeLa cells[1].
MS177 (0.1-5 μM, 16 h) effectively degrades cellular EZH2-PRC2 and suppresses global H3K27me3 in EOL-1 cells[1].
MS177 (0.1-5 μM, 16 h) induces Myc degradation in EOL-1 and MV4 cells[1].
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[1].
MS177 (0.5-2.5 μM, 24 h) decreases colony-forming capabilities in MV4;11 cells[1].
MS177 (0.5-2.5 μM, 24 h) slows cell cycle progression and induces MOLM-13 cell apoptosis[1].

Cell Viability Assay[1]

Cell 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 IC50s 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 Analysis[1]

Cell 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.
体内研究
(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[1].
MS177 (50 mg/kg, i.p.) achieves intraplasma concentrations about 1 μM in male Swiss Albino mice[1].
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[1].

Animal Model:PDX animal model of MLL-r AML[1]
Dosage:100 mg/kg
Administration:Intraperitoneal injection (i.p.), BID for 6 days.
Result:Inhibited tumor growth and prolonged survival.
分子量

914.02

性状

Solid

Formula

C48H55N11O8

CAS 号

2225938-86-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL(136.76 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.0941 mL5.4703 mL10.9407 mL
5 mM0.2188 mL1.0941 mL2.1881 mL
10 mM0.1094 mL0.5470 mL1.0941 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: 2.08 mg/mL (2.28 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (2.28 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。