Cat. No.: HY-130122

MG-277

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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.

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Pureté: 98.68%
CAS No.: 2411085-89-5
Formule: C₄₁H₄₂Cl₂FN₅O₅
Masse moléculaire:774.71

Stockage:

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Cereblon

Voir tous les produits spécifiques à Isoform PROTACs :

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.

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.

Chemical Information

CAS No. 2411085-89-5
Appearance Solid
Masse moléculaire 774.71
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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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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

Solvant et solubilité

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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:

Dosage Dosage
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (251 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[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

Keywords

MG-277

1 Cited Publications

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MG-277

PROTAC Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MG-277

Voir tous les produits spécifiques à Isoform PROTACs

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MG-277

PROTAC Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MG-277

Voir tous les produits spécifiques à Isoform PROTACs

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MG-277 Related Classifications

HY-130122 Related Classifications