PF-06821497 (b)( PF06821497 )

Catalog No. M12850 CAS No. 1844849-11-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PF-06821497 (b)
Note

Research use only, not for human use.
Brief Description

PF-06821497 (PF06821497) is a novel potent, selective, orally bioavailable EZH2 inhibitor.
Description

PF-06821497 (PF06821497) 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; weakly inhibits EZH1 (Ki=70 nM) and no significant affinity against a panel of other HMTases; inhibits Karpas-422 cell proliferation with IC50 of 23 nM, cell H3K27me3 IC50 of 17 nM; shows robust tumor growth inhibition in vivo.
In Vitro

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In Vivo

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Synonyms

PF06821497
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

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Indication

——

CAS Number

1844849-11-1
Formula Weight

467.343
Molecular Formula

C22H24Cl2N2O5
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

COC1=C(CN2CCC(C(Cl)=CC([C@@H](OC)C3COC3)=C4Cl)=C4C2=O)C(NC(C)=C1)=O
Chemical Name

(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

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

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