PF-06821497 | EZH2 Y641N inhibitor | Probechem Biochemicals

Chemical Structure : PF-06821497

CAS No.: 1844849-10-0

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PF-06821497 (PF 06821497)

货号: 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.

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5 mg	￥2280	In stock
10 mg	￥3680	In stock
25 mg	￥5980	In stock
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100 mg		Get quote

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生物&药学活性

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).

物理化学性质&存储条件

分子量	467.343
分子式	C22H24Cl2N2O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

1. Kung PP, et al. J Med Chem. 2018 Feb 8;61(3):650-665.

PF-06821497 (PF 06821497)

生物&药学活性

物理化学性质&存储条件

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PF-06821497 (PF 06821497)

生物&药学活性

物理化学性质&存储条件

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