EED226 |
| Catalog No.GC19130 |
EED226 es un inhibidor del complejo represivo Polycomb 2 (PRC2), que se une al bolsillo K27me3 en el desarrollo del ectodermo embrionario (EED) y muestra una fuerte actividad antitumoral en el modelo de ratones con xenoinjerto. EED226 es un inhibidor de EED potente, selectivo y biodisponible por vÍa oral. EED226 inhibe PRC2 con una IC50 de 23,4 nM cuando se utiliza el péptido H3K27me0 como sustrato en los ensayos enzimÁticos in vitro.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2083627-02-3
Sample solution is provided at 25 µL, 10mM.
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EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
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].
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)[1].
References:
[1]. Huang Y, et al. Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy. J Med Chem. 2017 Mar 23;60(6):2215-2226.
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