(R)-OR-S1 |CAS:1809336-19-3 Probechem Biochemicals

Chemical Structure : (R)-OR-S1

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(R)-OR-S1

货号: 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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生物&药学活性

(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.

物理化学性质&存储条件

分子量	532.479
分子式	C26H34BrN3O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2R)-7-Bromo-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-2-[trans-4-(dimethylamino)cyclohexyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide

参考文献

1. Honma D, et al. Cancer Sci. 2017 Oct;108(10):2069-2078.

(R)-OR-S1

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