MG-277

Name: MG-277
Brand: MedChemExpress
SKU: HY-130122
Rating: 4.5 (1 reviews)

Cat. No.: HY-130122 Purity: 98.66%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

MG-277 Chemical Structure

CAS No. : 2411085-89-5

Size	Price	Stock	Quantity
1 mg	USD 841	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1850	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 3000	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 5000	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Cereblon

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.

Molecular Weight

774.71

Formula

C₄₁H₄₂Cl₂FN₅O₅

CAS No.

2411085-89-5

Appearance

Solid

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.66%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (250 KB) RP-HPLC (249 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]

Complete Stock Solution Preparation Table

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

MG-277 Related Classifications

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

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

MG-277

Customer Review

MG-277 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

MG-277 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

MG-277 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report