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Chemical Structure : PF-06821497 S enantiomer
Catalog No.: PC-60001Not For Human Use, Lab Use Only.
PF-06821497 S enantiomer is a novel potent, selective, orally bioavailable EZH2 inhibitor with Ki of <0.1 and 1.15 nM aginast both wt and mutant Y641N EZH2, respectively.
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PF-06821497 S enantiomer is a novel potent, selective, orally bioavailable EZH2 inhibitor with Ki of <0.1 and 1.15 nM aginast both wt and mutant Y641N EZH2, respectively.
PF-06821497 weakly inhibits EZH1 (Ki=70 nM) and no significant affinity against a panel of other HMTases.
PF-06821497 inhibits Karpas-422 cell proliferation with IC50 of 23 nM, cell H3K27me3 IC50 of 17 nM; shows robust tumor growth inhibition in vivo.
| M.Wt | 467.343 | |
| Formula | C22H24Cl2N2O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kung PP, et al.J Med Chem. 2017 Dec 6. doi: 10.1021/acs.jmedchem.7b01375.
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