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Chemical Structure : (R)-OR-S1
Catalog No.: PC-60541Not For Human Use, Lab Use Only.
(R)-OR-S1 is a potent, selective, orally bioavailable EZH1/2 dual inhibitor with IC50 of 7.4/10 nM, inhibits H3K27me3 in HCT116 cells with IC50 of 0.47 nM.
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(R)-OR-S1 is a potent, selective, orally bioavailable EZH1/2 dual inhibitor with IC50 of 7.4/10 nM, inhibits H3K27me3 in HCT116 cells with IC50 of 0.47 nM.
(R)-OR-S1 strongly inhibited both EZH1 and EZH2, but not other methyltransferase, also potently inhibited EZH2 (Y641F) with IC50 of <10 nM.
(R)-OR-S1 showed greater antitumor efficacy than EZH2 selective inhibitor against KARPAS‐422 cells harboring a GOF mutation Y641N in EZH2, inhibited the growth of KARPAS‐422 cells in a dose‐dependent manner with GI50 of 4.0 nM.
(R)-OR-S1 efficacy against some lymphomas, multiple myeloma, and leukemia with fusion genes such as MLL-AF9, MLL-AF4, and AML1-ETO.
(R)-OR-S1 demonstrated antitumor activities in xenograft models of against rhabdoid tumor cell line G401 and gastric cancer cell line NCI‐N87.
| M.Wt | 532.479 | |
| Formula | C26H34BrN3O4 | |
| Appearance | Solid | |
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| Solubility |
10 mM in DMSO |
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1. Honma D, et al. Cancer Sci. 2017 Oct;108(10):2069-2078.
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