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PF-06821497 Chemical Structure

PF-06821497

Data Sheet For research use only. Not for human use.
Cat. No. :BCP45826CAS No. :1844849-10-0Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 1844849-10-0 Cat. No. BCP45826
Name PF-06821497
Synonyms PF06821497;PF 06821497;
SMILES CC1=CC(=C(C(=O)N1)CN2CCC3=C(C=C(C(=C3C2=O)Cl)C(C4COC4)OC)Cl)OC
Chemical Name
Formula C22H24Cl2N2O5 M. Wt 467.34
Purity 98% Storage Store at 4-8°C
Description 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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