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EED226
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EED226
CAS No. : 2083627-02-3
MCE 站:EED226
产品活性:EED226 是一种多梳抑制复合物 2 (PRC2) 抑制剂,与胚胎外胚层发育 (EED) 上的 K27me3 口袋结合,在移植瘤小鼠模型中具有强的抗肿瘤活性。EED226 是一种有效的,口服可生物利用的,选择性 EED 抑制剂。当 H3K27me0 肽用作体外酶法测定的底物时,EED226 抑制 PRC2 的 IC50 为 23.4 nM。
研究领域:Epigenetics
作用靶点:Histone Methyltransferase
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.
In the in vitro enzymatic assays, EED226 inhibited PRC2 with an IC50 of 53.5 nM when the mononucleosome is used as the substrate, with the stimulatory H3K27me3 added at 1× Kact (1.0 μM).
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).
相关产品:Bioactive Compound Library Plus | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Reprogramming Compound Library | Orally Active Compound Library | Anti-Blood Cancer Compound Library | 3-Deazaneplanocin A hydrochloride | Chaetocin | UNC0642 | UNC1999 | MS023 | BIX-01294 | EPZ020411 hydrochloride | MM-102 TFA | SGC0946 | A-366 | Amodiaquine dihydrochloride dihydrate | CM-272 | AZ505 | SGC707 | PFI-2 hydrochloride | NSC 663284 | UNC0379 | A-196 | Sinefungin | SGC3027 | AMI-1 | EI1 | BVT948 | MS049 | HLCL-61 hydrochloride | UNC0646 | UNC 0631 | UNC3866
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