Information MS1943 MS1943 is an orally bioavailable EZH2 selective degrader with IC50 of 120 nM. Targets EZH2 (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. 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. Cell Research(from reference) 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
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MS1943
CAS number：2225938-17-8 molecular formula：C42H54N8O3
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| Chinese alias | - | ||
| English alias | 6-(6-(4-(2-(2-((3r,5r,7r)-damantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide | ||
| CAS number | 2225938-17-8 | molecular formula | C42H54N8O3 |
| molecular weight | 718.93 g/mol | Exact mass | ≥98% |
| PSA | 124.000 Ų | logp | 4.773 |
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