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Dot1L-IN-4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dot1L-IN-4图片
CAS NO:2565705-02-2
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Dot1L-IN-4 是一种有效的类端粒沉默干扰体 1 (DOT1L) 抑制剂,IC50 SPA DOT1L 为 0.11 nM。
Cas No.2565705-02-2
分子式C28H27ClF2N8O5S
分子量661.08
溶解度DMSO : 250 mg/mL (378.17 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM[1].

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].

[1]. FrÉdÉric Stauffer, et al. New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse. ACS Med. Chem. Lett. 2019, 10, 12, 1655-1660.