1940206-71-2
1940206-71-2 结构式
基本信息
中文别名
化合物 T11082 英文别名
Dot1L-IN-22,4-Pyrimidinediamine, N4-methyl-N2-[2-methyl-1-[2-[(3-methyl-3H-imidazo[4,5-b]pyridin-6-yl)oxy]phenyl]-1H-indol-6-yl]-
物理化学性质
沸点681.6±65.0 °C(Predicted)
密度1.36±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)6.81±0.10(Predicted)
常见问题列表
生物活性
Dot1L-IN-2 是一种有效的，选择性的，可口服的 Dot1L (一种 histone methyltransferase)，IC50 值和 Ki 值分别为 0.4 nM 和 0.08 nM。靶点
IC50: 0.4 nM (Dot1L)
Ki: 0.08 nM (Dot1L)
体外研究
Dot1L-IN-2 is a potent, selective Dot1L inhibitor, with an IC 50 and K i of 0.4 nM and 0.08 nM, respectively. Dot1L-IN-2 potently inhibits H3K79 dimethylation (IC 50 , 16 nM), and blocks the activity of the HoxA9 promoter (IC 50 , 340 nM) in cellular systems. Dot1L-IN-2 also dramatically suppresses proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC 50 , 128 nM).