EED226

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

CAS号 ：2083627-02-3

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 EZH2^MUT 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 t_1/2 (2.2 h), and moderate plasma protein binding (PPB)


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