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EED226
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EED226图片
CAS NO:2083627-02-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)369.40
FormulaC17H15N5O3S
CAS No.2083627-02-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 73 mg/mL (197.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILESO=S(C1=CC=C(C2=CN=C(NCC3=CC=CO3)N4C2=NN=C4)C=C1)(C)=O
SynonymsEED226; EED-226; EED 226
实验参考方法
In Vitro

In vitro activity: EED226 is a highly potent, efficient and selective inhibitor of EZH2 and EZH1 evaluated against a broad range of epigenetic and non-epigenetic targets. It potently reduces global H3K27Me3 mark in cells and demonstrates selectively cell killing effects in cells carrying a heterozygous Y641N mutation. EED226 has moderate permeability as the measured in Caco-2 cells at A→B=3.0x10-6 cm/s, with an efflux ratio at 7.6.


Kinase Assay: EED226 is a highly potent, efficient and selective inhibitor of EZH2 and EZH1 evaluated against a broad range of epigenetic and non-epigenetic targets. It potently reduces global H3K27Me3 mark in cells and demonstrates selectively cell killing effects in cells carrying a heterozygous Y641N mutation. EED226 has moderate permeability as the measured in Caco-2 cells at A→B=3.0x10-6 cm/s, with an efflux ratio at 7.6.


Cell Assay: G401 cells are treated with EED226 for 3 d at the indicated concentrations. Total histone H3 is shown as a loading control. WB analysis for protein expression of H3K27me3, H3K27me2, H3K27me1.

In VivoEED226 induces robust and sustained tumor regression in EZH2MUT pre-clinical DLBCL model. In CD-1 mice, dosing of EED226 for 14 days at 300 mg/kg bid is well tolerated with no apparent adverse effects. It has very low in vivo clearance, and approximately 100% oral bioavailability. EED226 has low volume of distribution (0.8 L/kg), reasonable terminal t1/2 (2.2 h), and moderate plasma protein binding (PPB).
Animal modelKarpas422 xenograft tumors (mouse model)
Formulation & DosageDissolved in 75% Soluplus + 5% sodium laureth sulfate + 20% EED226; 10 ml/kg ; Oral gavage
ReferencesNat Chem Biol. 2017 Apr;13(4):381-388; Cancer Discov. 2017 Apr;7(4):OF8.