1809336-19-3
1809336-19-3 structure
- Name: (R)-OR-S1
- Chemical Name: (R)-OR-S1
- CAS Number: 1809336-19-3
- Molecular Formula: C26H34BrN3O4
- Molecular Weight: 532.479
- Create Date: 2020-01-12 12:01:50
- Modify Date: 2024-01-20 21:14:01
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A novel SAM-competitive, highly selective, orally bioavailable EZH1/2 dual inhibitor with IC50 of 16/50 nM, respectively; also inhibits EZH2 Y641N mutant (IC50=50 nM), shows no significant activity against a panel of 253 kinases; show greater antitumor efficacy than EZH2 selective inhibitor against KARPAS-422 cells harboring a GOF mutation in EZH2, also more potently reduced H3K27me3 in cells than EZH2 selective inhibitors.
| Name | (R)-OR-S1 |
|---|
| Description | A novel SAM-competitive, highly selective, orally bioavailable EZH1/2 dual inhibitor with IC50 of 16/50 nM, respectively; also inhibits EZH2 Y641N mutant (IC50=50 nM), shows no significant activity against a panel of 253 kinases; show greater antitumor efficacy than EZH2 selective inhibitor against KARPAS-422 cells harboring a GOF mutation in EZH2, also more potently reduced H3K27me3 in cells than EZH2 selective inhibitors. |
|---|---|
| References | References 1. Honma D, et al. Cancer Sci. 2017 Oct;108(10):2069-2078. View Related Products by Target Histone Methyltransferase (HMTase) |
| Molecular Formula | C26H34BrN3O4 |
|---|---|
| Molecular Weight | 532.479 |