Dot1L-IN-4 MedChemExpress (MCE)

Product Name	Dot1L-IN-4
Synonyms	QQN05022 Dot1L-IN-4 Dot1L- IN-4 QQN05022(Dot1L-IN-4) N1-[(3-Chloro-pyridin-2-yl)-(2,2-difluoro-benzo[1,3]dioxol-4-yl)-methyl]-4-methanesulfonyl-N2-(4-methoxy-6-piperazin-1-yl-[1,3,5]triazin-2-yl)-benzene-1,2-diamine Synonyms QQN05022 Dot1L-IN-4 Dot1L- IN-4 QQN05022(Dot1L-IN-4) N1-[(3-Chloro-pyridin-2-yl)-(2,2-difluoro-benzo[1,3]dioxol-4-yl)-methyl]-4-methanesulfonyl-N2-(4-methoxy-6-piperazin-1-yl-[1,3,5]triazin-2-yl)-benzene-1,2-diamine 1,2-Benzenediamine, N1-[(S)-(3-chloro-2-pyridinyl)(2,2-difluoro-1,3-benzodioxol-4-yl)methyl]-N2-[4-methoxy-6-(1-piperazinyl)-1,3,5-triazin-2-yl]-4-(methylsulfonyl)-
CAS	2565705-02-2
EINECS
Chemical Formula	C28H27ClF2N8O5S
Molecular Weight	661.08
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg
Price	Email to quote
Descriptions	Dot1L-IN-4 Dot1L-IN-4 MedChemExpress (MCE) HY-135127 2565705-02-2 99.54% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Dot1L-IN-4 Dot1L-IN-4 MedChemExpress (MCE) HY-135127 2565705-02-2 99.54% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM. Dot1L-IN-4 (Compound 10) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=1.7 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=33 nM). Dot1L-IN-4 also inhibits mixed lineage leukemia (MLL) with an IC50 of 99 µM[1]. Dot1L-IN-4 (Compound 10 300 mg/kg p.o. qd) is not tolerated at such a high dose by tumor xenograft bearing mice, and at a 6-fold reduced dose, the tumor growth as well as the HOXA9 reporter gene mRNA are reduced only by less than half as compared to control animals[1]. DOT1L 0.11 nM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Frédéric Stauffer, et al. New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse. ACS Med. Chem. Lett. 2019, 10, 12, 1655-1660.
Last Update	2025-04-01 14:45:47

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