PRC2 EED-IN-1

Chemical Structure : PRC2 EED-IN-1

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货号: PC-72291Not For Human Use, Lab Use Only.

PRC2 EED-IN-1 is a potent, selective, allosteric, orally bioavailable inhibitor of the EED subunit of histone methyltransferase PRC2 with IC50 of 44 nM (H3K27me3 inhibition).

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生物&药学活性

PRC2 EED-IN-1 is a potent, selective, allosteric, orally bioavailable inhibitor of the EED subunit of histone methyltransferase PRC2 with IC50 of 44 nM (H3K27me3 inhibition).
PRC2 EED-IN-1 retains efficacy against EZH2 inhibitor-resistant cell lines (Karpas 44 cell IC50=27 nM), exhibits in vivo efficacy in EZH2-driven tumors in vivo.

物理化学性质&存储条件

分子量	394.414
分子式	C19H19FN8O
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	N5-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-N8-methyl-N8-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-c]pyrimidine-5,8-diamine

参考文献

1. Bagal SK, et al. J Med Chem. 2021 Dec 9;64(23):17146-17183.

PRC2 EED-IN-1

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物理化学性质&存储条件

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PRC2 EED-IN-1

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