MS1943

Catalog No.S8918

For research use only.

MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity.

MS1943 Chemical Structure

CAS No. 2225938-17-8

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity.
Targets
EZH2 [1]
(Cell-free assay)
120 nM
In vitro

MS1943 is a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. MS1943 has a profound cytotoxic effect in multiple TNBC cells, while sparing normal cells. MS1943 mediates its cytotoxic effects through ER stress and UPR induction in cells that are dependent for their growth on EZH2.[1]

In vivo

MS1943 is efficacious in vivo and well tolerated in mice at the efficacious dose, suggesting that pharmacologic degradation of EZH2 can be advantageous for treating the cancers that are dependent on EZH2.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MDA-MB-468 cells, HCC70 cells, BT549, HCC70 and MDA-MB-231 TNBC cells, KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells
  • Concentrations: 5 μM, 4 μM
  • Incubation Time: 24 h, 6 h
  • Method:

    For the study using MDA-MB-468 cells, cells are cultured for 24 h in the presence of MS1943 (5 μM), alone or with different concentrations of the proteasome inhibitor MG132, and EZH2 protein levels are detected via western blot as described already. Vinculin is used as a loading control to normalize EZH2 protein levels. For the study using HCC70 cells, cells are cultured for 6 h in the presence of MS1943 (4 μM), alone or with different concentrations of MG132, and EZH2 protein levels are detected via western blot as described before. Actin is used as a loading control to normalize EZH2 protein levels.

Animal Research:

[1]

  • Animal Models: eight-week-old female BALB/c nude mice
  • Dosages: 150 mg/kg
  • Administration: IP

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(139.09 mM)
Ethanol 100 mg/mL
(139.09 mM)
Water Insoluble

Chemical Information

Molecular Weight 718.93
Formula

C42H54N8O3

CAS No. 2225938-17-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)CCNC(=O)CC67CC8CC(C6)CC(C8)C7)C(C)C)C

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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