产品信息
抗原名称
EED226
商品描述
EED226 is a potent and selective PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED.
分子量
369.40
纯度
>98%
可溶性
DMSO : ≥ 29 mg/mL
外观
Powder
In vitro(体外研究)
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.
In vivo(体内研究)
EED226 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).
背景
别名
EED226；EED 226；MAK683
分子式
C17H15N5O3S
CAS号
2083627-02-3
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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