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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $55 | - | In Stock | |
| 5 mg | $99 | - | In Stock | |
| 10 mg | $189 | - | In Stock | |
| 25 mg | $389 | - | In Stock | |
| 50 mg | $658 | - | In Stock | |
| 100 mg | $1,098 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $158 | - | In Stock |
| 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]. |
| Molecular Weight | 718.93 |
| Formula | C42H54N8O3 |
| Cas No. | 2225938-17-8 |
| Smiles | CC(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 | keep away from direct sunlight | Powder: -20°C for 3 years | 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
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