MS1943

Catalog No.S8918 Batch:S891802

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Technical Data

Formula

C42H54N8O3
Molecular Weight 718.93 CAS No. 2225938-17-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (139.09 mM)
Ethanol 100 mg/mL (139.09 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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 Assay:

[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 Study:

[1]
  • Animal Models

    eight-week-old female BALB/c nude mice

  • Dosages

    150 mg/kg

  • Administration

    IP

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.