EED226

EED226

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  • ¥500
  • 喀露蓝
  • 上海
  • CPDB1019
  • 2025年07月10日
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    上海喀露蓝科技技术有限公司
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    • 详细信息
    • 技术资料
    • 保质期：

      2年

    • 英文名：

      Furan-2-ylmethyl-[8-(4-methanesulfonyl-phenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-yl]-amine

    • 库存：

      现货 1mg-100g-1kg

    • 供应商：

      喀露蓝

    • 规格：

      98% min

    EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM. IC50 & Target: IC50: 22 nM (EED226)[1] 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=3.0x10-6 cm/s, with an efflux ratio at 7.6[1]. In Vivo: 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)


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    EED226
    ¥500