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MS1943

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Catalog No. T13780Cas No. 2225938-17-8

MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).

MS1943

MS1943

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Purity: 95.82%
Catalog No. T13780Cas No. 2225938-17-8
MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$35-In Stock
2 mg$50-In Stock
5 mg$81-In Stock
10 mg$139-In Stock
25 mg$277-In Stock
50 mg$488-In Stock
100 mg$890-In Stock
200 mg$1,470-In Stock
1 mL x 10 mM (in DMSO)$129-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:95.82%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
Targets&IC50
EZH2:120 nM
In vitro
MS1943 inhibits cell growth (GI50 of 2.2 μM). MS1943 induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells[1].
In vivo
A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 μM and resulted in plasma concentrations above its cellular IC50 value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 μM, but plasma concentrations were below the cellular IC50 value.MS1943 suppresses tumor growth[1].
Chemical Properties
Molecular Weight718.93
FormulaC42H54N8O3
Cas No.2225938-17-8
SmilesCC(C)n1ncc2c(cc(cc12)-c1ccc(nc1)N1CCN(CCNC(=O)CC23CC4CC(CC(C4)C2)C3)CC1)C(=O)NCc1c(C)cc(C)[nH]c1=O
Relative Density.1.36 g/cm3 (Predicted)
Storage & Solubility Information
Storagekeep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 120 mg/mL (166.91 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (6.95 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.3910 mL6.9548 mL13.9096 mL69.5478 mL
5 mM0.2782 mL1.3910 mL2.7819 mL13.9096 mL
10 mM0.1391 mL0.6955 mL1.3910 mL6.9548 mL
20 mM0.0695 mL0.3477 mL0.6955 mL3.4774 mL
50 mM0.0278 mL0.1391 mL0.2782 mL1.3910 mL
100 mM0.0139 mL0.0695 mL0.1391 mL0.6955 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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