DOT1L R231Q inhibitor 37

Chemical Structure : DOT1L R231Q inhibitor 37

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货号: PC-22999Not For Human Use, Lab Use Only.

DOT1L R231Q inhibitor 37 is a first-in-class DOT1L R231Q inhibitor, inhibits proliferation of H460 cells expressing DOT1LR231Q with IC50 of 6.18 uM.

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250 mg		Get quote

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生物&药学活性

DOT1L R231Q inhibitor 37 is a first-in-class DOT1L R231Q inhibitor, inhibits proliferation of H460 cells expressing DOT1LR231Q with IC50 of 6.18 uM.
DOT1L R231Q inhibitor 37 exhibits remarkably weaker inhibitory activity of DOT1LWT (IC50=2.08 uM) compare to SGC0946.
DOT1L R231Q inhibitor 37 decreases H3K79me2 level, while H3K27me3, H3K9me2, H3K4me1 and H3K36me2 levels remained relatively unchanged.
DOT1L R231Q inhibitor 37 inhibited colony formation in H460R231Q, H1299R231Q, H1975R231Q, and H446R231Q lung cancer cells.
DOT1L R231Q inhibitor 37 demonstrates in vivo antitumor activity in H460WT/R231Q OE CDX model.

物理化学性质&存储条件

分子量	705.87
分子式	C35H51N11O5
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	N-(2-((4-((((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(3-morpholinopropyl)amino)piperidin-1-yl)methyl)-1H-benzo[d]imidazol-6-yl)pivalamide

参考文献

1. Zehui Tan, et al. Acta Pharm Sin B. 2024 Aug;14(8):3605-3623.