EED226 |
| カタログ番号GC19130 |
EED226 はポリコーム抑制複合体 2 (PRC2) 阻害剤であり、胚性外胚葉発生 (EED) の K27me3 ポケットに結合し、異種移植マウスモデルで強力な抗腫瘍活性を示します。 EED226 は、強力で、選択的で、経口的に生物学的に利用可能な EED 阻害剤です。 EED226 は、in vitro 酵素アッセイで H3K27me0 ペプチドを基質として使用した場合、23.4 nM の IC50 で PRC2 を阻害します。
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.
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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