MS177|cas:2225938-86-1|西域试剂

MS177,98.00%

产品编号：Bellancom-148333| CAS NO：2225938-86-1| 分子式：C₄₈H₅₅N₁₁O₈| 分子量：914.02

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-148333	￥2400.00	杭州北京（现货）
Bellancom-148333	￥3800.00	杭州北京（现货）
Bellancom-148333	￥7500.00	杭州北京（现货）
Bellancom-148333	￥12000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

MS177

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 (C24 IC₅₀: 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-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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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.
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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	1.0941 mL	5.4703 mL	10.9407 mL
5 mM	0.2188 mL	1.0941 mL	2.1881 mL
10 mM	0.1094 mL	0.5470 mL	1.0941 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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