MG-277

目录号: HY-130122 纯度: 98.66%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

MG-277 是一种分子胶降解剂，可基于Cereblon E3配体有效诱导翻译终止因子 GSPT1 的降解，DC₅₀ 为 1.3 nM。MG-277 以非 p53 的方式高度有效地抑制肿瘤细胞的生长，对 RS4; 11 细胞和 p53 突变体 RS4;11/IRMI-2 细胞的 IC₅₀ 分别为 3.5 nM 和 3.4 nM。MG-277 具有有效的抗癌活性。

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MG-277 Chemical Structure

CAS No. : 2411085-89-5

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1 mg	￥7400	In-stock
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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

生物活性
纯度 & 产品资料
参考文献

生物活性

MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC₅₀ of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC₅₀s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity^[1].

IC₅₀ & Target^[1]

Cereblon

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	8.3 nM Compound: MG-277	Antiproliferative activity against human HL60 cells with lack of p53 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human HL60 cells with lack of p53 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	> 3 μM Compound: MG-277	Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	> 3 μM Compound: MG-277	Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	0.03 μM Compound: MG-277	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	1372 nM Compound: MG-277	Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 30 uM of lenalidomide Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 30 uM of lenalidomide	[PMID: 31560543]
MDA-MB-231	IC₅₀	19.3 nM Compound: MG-277	Antiproliferative activity against human MDA-MB-231 cells transfected with MDM2 siRNA assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells transfected with MDM2 siRNA assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	2138 nM Compound: MG-277	Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 100 uM of lenalidomide Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 100 uM of lenalidomide	[PMID: 31560543]
MDA-MB-231	IC₅₀	28.9 nM Compound: MG-277	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 2 days followed by compound treatment by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 2 days followed by compound treatment by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	32.2 nM Compound: MG-277	Binding affinity to cereblon in human MDA-MB-231 cells assessed as cell growth inhibition measured after 4 days Binding affinity to cereblon in human MDA-MB-231 cells assessed as cell growth inhibition measured after 4 days	[PMID: 31560543]
MDA-MB-231	IC₅₀	39.4 nM Compound: MG-277	Antiproliferative activity against human MDA-MB-231 cells harboring mutant p53 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells harboring mutant p53 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	39.4 nM Compound: MG-277	Antiproliferative activity against human MDA-MB-231 cells harboring mutant p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells harboring mutant p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	623.1 nM Compound: MG-277	Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 10 uM of lenalidomide Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 10 uM of lenalidomide	[PMID: 31560543]
MDA-MB-468	IC₅₀	> 1 μM Compound: MG-277	Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	> 1 μM Compound: MG-277	Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	0.062 μM Compound: MG-277	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	19.8 nM Compound: MG-277	Antiproliferative activity against human MDA-MB-468 cells transfected with MDM2 siRNA assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells transfected with MDM2 siRNA assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	2072 nM Compound: MG-277	Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 100 uM lenalidomide Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 100 uM lenalidomide	[PMID: 31560543]
MDA-MB-468	IC₅₀	26.4 nM Compound: MG-277	Antiproliferative activity against human MDA-MB-468 cells harboring mutant p53 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells harboring mutant p53 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	26.4 nM Compound: MG-277	Antiproliferative activity against human MDA-MB-468 cells harboring mutant p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells harboring mutant p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	28.7 nM Compound: MG-277	Binding affinity to cereblon in human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 days Binding affinity to cereblon in human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 days	[PMID: 31560543]
MDA-MB-468	IC₅₀	31.1 nM Compound: MG-277	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 2 days followed by compound treatment by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 2 days followed by compound treatment by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	418.9 nM Compound: MG-277	Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 10 uM lenalidomide Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 10 uM lenalidomide	[PMID: 31560543]
MDA-MB-468	IC₅₀	963.9 nM Compound: MG-277	Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 30 uM lenalidomide Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 30 uM lenalidomide	[PMID: 31560543]
MOLM-13	IC₅₀	24.6 nM Compound: MG-277	Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MV4-11	IC₅₀	7.8 nM Compound: MG-277	Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
RS4-11	IC₅₀	0.17 nM Compound: MG-277	Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay	[PMID: 31560543]
RS4-11	IC₅₀	2.3 nM Compound: MG-277	Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as MDM2-independent cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as MDM2-independent cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
RS4-11	IC₅₀	3.5 nM Compound: MG-277	Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]

体外研究
(In Vitro)

MG-277 (0.03-10 nM；24 小时；RS4；11 细胞) 处理可抑制细胞生长并降解 GSPT1^[1]。
MG277 在降低细胞中 MDM2 蛋白水平方面的效力显著降低，并且无法激活野生型 p53。MG-277 在具有野生型 p53、突变型 p53 或缺失型 p53 的癌细胞系中具有很强的抑制细胞生长的能力，表明其是一种 p53 非依赖性机制。MG-277 以 p53 和 MDM2 非依赖性方式诱导癌细胞中 GSPT1 快速降解，但方式依赖于 cereblon、CUL4 E3 泛素连接酶和蛋白酶体^[1]。

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

Western Blot Analysis^[1]

Cell Line:	RS4;11 cells
Concentration:	0.03 nM, 0.1 nM, 0. 3 nM, 1 nM, 3 nM, 10 nM
Incubation Time:	24 hours
Result:	Degraded GSPT1.

分子量

774.71

Formula

C₄₁H₄₂Cl₂FN₅O₅

CAS 号

2411085-89-5

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (64.54 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2908 mL	6.4540 mL	12.9081 mL
5 mM	0.2582 mL	1.2908 mL	2.5816 mL
10 mM	0.1291 mL	0.6454 mL	1.2908 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (6.45 mM); 悬浊液; 超声助溶

此方案可获得 5 mg/mL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 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (6.45 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.66%

选择批次：

Data Sheet (638 KB) SDS (251 KB)

COA (287 KB) RP-HPLC (249 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Yang J, et al. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders. J Med Chem. 2019 Oct 21. [Content Brief]

MG-277 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.2908 mL	6.4540 mL	12.9081 mL	32.2701 mL
	5 mM	0.2582 mL	1.2908 mL	2.5816 mL	6.4540 mL
	10 mM	0.1291 mL	0.6454 mL	1.2908 mL	3.2270 mL
	15 mM	0.0861 mL	0.4303 mL	0.8605 mL	2.1513 mL
	20 mM	0.0645 mL	0.3227 mL	0.6454 mL	1.6135 mL
	25 mM	0.0516 mL	0.2582 mL	0.5163 mL	1.2908 mL
	30 mM	0.0430 mL	0.2151 mL	0.4303 mL	1.0757 mL
	40 mM	0.0323 mL	0.1614 mL	0.3227 mL	0.8068 mL
	50 mM	0.0258 mL	0.1291 mL	0.2582 mL	0.6454 mL
	60 mM	0.0215 mL	0.1076 mL	0.2151 mL	0.5378 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MG-2772411085-89-5MG277MG 277Molecular GluesPROTACsApoptosisCancercellgrowthPROTACMDM2GSPT1degradationmolecularglueInhibitorinhibitorinhibit

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MG-277

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完整储备液配制表

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MG-277

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摩尔计算器

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完整储备液配制表

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