2. PROTAC Apoptosis
  3. Molecular Glues PROTACs Apoptosis
  4. MG-277

MG-277 

Cat. No.: HY-130122 Purity: 98.66%
COA Handling Instructions

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

MG-277 Chemical Structure

CAS No. : 2411085-89-5

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10 mg USD 3000 In-stock
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Based on 1 publication(s) in Google Scholar

MG-277 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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

 

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].

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

MG-277 Related Antibodies

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

Appearance

Solid

Formula

C41H42Cl2FN5O5
CAS No.
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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.66%

COA (254 KB) RP-HPLC (249 KB)

Handling Instructions (2659 KB)
References
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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.

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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

Keywords:

MG-2772411085-89-5MG277MG 277Molecular GluesPROTACsApoptosisCancercellgrowthPROTACMDM2GSPT1degradationmolecularglueInhibitorinhibitorinhibit

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