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Chemical Structure : PF-06821497
CAS No.: 1844849-10-0
Catalog No.: PC-72620Not For Human Use, Lab Use Only.
PF-06821497 (PF 06821497) is a potent, selective, orally bioavailable Enhancer of Zeste Homolog 2 (EZH2) inhibitor with Ki of <1 nM against Y641N mutant.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $368 | In stock | |
| 25 mg | $598 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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PF-06821497 (PF 06821497) is a potent, selective, orally bioavailable Enhancer of Zeste Homolog 2 (EZH2) inhibitor with Ki of <1 nM against Y641N mutant.
PF-06821497 demonstrates high selectivity in the CEREP histone methyltransferase and broad-ligand screening panels, with exception EZH1 (Ki=70 nM), does not impair the function of various cytochrome P450 (CYPs) isoforms (IC50>30 uM) and does not exhibit appreciable inhibition of hERG ion channel.
PF-06821497 significantly reduced H3K27me3 levels in mice bearing Karpas-422 DLBCL tumor xenografts (which contain the Y641N EZH2 mutation).
| M.Wt | 467.343 | |
| Formula | C22H24Cl2N2O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-5,8-dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one |
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1. Kung PP, et al. J Med Chem. 2018 Feb 8;61(3):650-665.
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