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PF-06821497 S enantiomer

Chemical Structure : PF-06821497 S enantiomer

CAS No.: 1844849-11-1

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PF-06821497 S enantiomer (PF06821497 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 467.343
Formula C22H24Cl2N2O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-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

References

1. Kung PP, et al.J Med Chem. 2017 Dec 6. doi: 10.1021/acs.jmedchem.7b01375.

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