Chemical Structure : DOT1L R231Q inhibitor 37
CAS No.:
DOT1L R231Q inhibitor 37
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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705.87
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Formula
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C35H51N11O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Zehui Tan, et al. Acta Pharm Sin B. 2024 Aug;14(8):3605-3623.
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