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MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 52 € | In Stock | |
5 mg | 94 € | In Stock | |
10 mg | 179 € | In Stock | |
25 mg | 369 € | In Stock | |
50 mg | 625 € | In Stock | |
100 mg | 1.043 € | In Stock | |
1 mL x 10 mM (in DMSO) | 150 € | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 120 mg/mL (166.91 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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