CAS NO: | 2083627-02-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model[1]. EED226 is a potent, selective, and orally bioavailable EED inhibitor[2]. EED226 inhibitsPRC2with anIC50of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays[3]. | ||||||||||||||||
IC50& Target | IC50: 23.4 nM (PRC2)[3] | ||||||||||||||||
体外研究 (In Vitro) | 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=3.0x10-6cm/s, with an efflux ratio at 7.6[2]. | ||||||||||||||||
体内研究 (In Vivo) | EED226 induces robust and sustained tumor regression in EZH2MUTpre-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 lowin vivoclearance, 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)[2]. | ||||||||||||||||
分子量 | 369.40 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H15N5O3S | ||||||||||||||||
CAS 号 | 2083627-02-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 125 mg/mL(338.39 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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