Cat. No.: HY-130122

MG-277

Name: MG-277
Brand: MedChemExpress
SKU: HY-130122
Price: 323.00 USD
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Based on 1 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity : 98.68%
CAS No.: 2411085-89-5
Formula: C₄₁H₄₂Cl₂FN₅O₅
Molecular Weight:774.71

Storage:

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

MG-277 Chemical Structure

CAS No.: 2411085-89-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Protocols (6)
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

eRF3a/GSPT1

All Eukaryotic Release Factor (eRF) Isoforms :

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]

In Vitro

MG-277 (0.03-10 nM; 24 hours; RS4;11 cells) treatment inhibits cell growth and degrades GSPT1^[1].
MG277 has a significantly decreased potency in reducing the level of MDM2 protein in cells and fails to activate wild-type p53. MG-277 is highly potent and effective in inhibition of cell growth in cancer cell lines with wild-type p53, mutated p53, or deleted p53, indicating a p53-independent mechanism. MG-277 induces rapid GSPT1 degradation in cancer cells in a p53- and MDM2-independent manner but in a manner dependent upon cereblon, CUL4 E3 ubiquitin ligase, and proteasomes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

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.

Chemical Information

CAS No. 2411085-89-5
Appearance Solid
Molecular Weight 774.71
Formula C₄₁H₄₂Cl₂FN₅O₅
Color White to off-white
SMILES

ClC1=CC=C2C(NC([C@@]23C4(N[C@H]([C@@H]3C5=CC=CC(Cl)=C5F)C(NCCCCCC6=C(C7=CC=C6)CN(C7=O)C8C(NC(CC8)=O)=O)=O)CCCCC4)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (1)

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Journal Impact Factor

Nat Commun

PROTAC repurposing uncovers a noncanonical binding surface that mediates chemical degradation of nuclear receptors. [Abstract]

2025 Nov 6;16(1):9805. PMID: 41198675

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (64.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

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Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 5 mg/mL (6.45 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (6.45 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocols

All Cell Biology

Protocol for Cell Counting and Cell Density Analysis
Cell counting and cell-density analysis estimate the number of cells in a known volume or field area. Manual hemocytometer counting uses a chamber of defined geometry to convert counted cells into cells/mL, while automated counters and image-analysis workflows detect cell objects from optical, brightfield, fluorescence, impedance, or digital-image features. Trypan blue viability counting is based on dye exclusion: viable cells with intact membranes exclude dye, while non-viable cells with compromised membranes stain blue. The readout is total cell density, viable-cell density, dead-cell density, and percent viability. Cell density can also be estimated from microscopy images by counting objects per image area, from flow cytometry using calibrated volume or reference particles, or from in situ microscopy in bioreactors after calibration against reference methods such as hemocytometer or flow cytometry.
Somatic Cell Culture
A method of simulating the in vivo environment in vitro to maintain the cell growth, differentation and main functions.
CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
Cell Counting-Based Growth Curve Assay
Cell counting-based growth curve assays quantify cell proliferation by directly measuring changes in viable cell number over time using manual or automated counting methods such as hemocytometer-based counting or instrument-assisted cell enumeration, enabling construction of growth curves that reflect population expansion dynamics in response to culture conditions. A widely used approach is trypan blue exclusion with hemocytometer counting, where membrane-compromised (non-viable) cells take up the dye, allowing discrimination between viable and non-viable cells while simultaneously enabling total cell number quantification. Repeated sampling across time points allows estimation of proliferation rate, growth phases, and comparative growth kinetics between experimental conditions.
MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

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MG-277

Publications Citing Use of MedChemExpress (MCE) MG-277

All Eukaryotic Release Factor (eRF) Isoforms