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1809336-19-3

1809336-19-3 structure
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: 2025-08-25 17:10:55
  • 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
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