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PF-06821497 结构式

PF-06821497

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货号 :BCP45826CAS号 :1844849-10-0纯度:98%
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  • 基本信息与产品描述
CAS号 1844849-10-0 货号 BCP45826
中文名 PF-06821497
英文名 PF-06821497
中文别名
英文别名 PF06821497;PF 06821497;
SMILES CC1=CC(=C(C(=O)N1)CN2CCC3=C(C=C(C(=C3C2=O)Cl)C(C4COC4)OC)Cl)OC
化学名称
分子式 C22H24Cl2N2O5 分子量 467.34
纯度 98% 配送 惯例下常温包邮
产品描述 EZH2 Inhibitor PF-06821497 is an orally available selective inhibitor of the histone lysine methyltransferase (HMT) enhancer of zeste homolog 2 (EZH2), with potential antineoplastic activity. Upon oral administration, EZH2 inhibitor PF-06821497 selectively targets, binds to and inhibits the activity of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells. EZH2, an HMT class enzyme and the catalytic subunit of the polycomb repressive complex 2 (PRC2), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation; its expression is correlated with tumor initiation, progression, stem cell self-renewal, migration and angiogenesis.
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