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UNC2250
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。
UNC2250图片
CAS NO:1493694-70-4
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
UNC2250 是一种有效的选择性 Mer 抑制剂，IC50 为 1.7 nM，比密切相关的激酶 Axl/Tyro3 的选择性高约 160 倍和 60 倍。
Cas No.1493694-70-4
别名反式-4-[[2-(丁基氨基)-5-[5-(4-吗啉基甲基)-2-吡啶基]-4-嘧啶基]氨基]环己醇
化学名4-[[2-(butylamino)-5-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-yl]amino]cyclohexan-1-ol
Canonical SMILESCCCCNC1=NC=C(C(=N1)NC2CCC(CC2)O)C3=NC=C(C=C3)CN4CCOCC4
分子式C24H36N6O2
分子量440.58
溶解度≥ 22.05mg/mL in DMSO with gentle warming
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

UNC2250 is a highly selective inhibitor of Mer receptor tyrosine kinase with IC50 value of 1.7nM [1].

UNC2250 shows a potent inhibitory activity against Mer with IC50 value of 1.7nM. The IC50 values for other TAM kinases such as Axl and Tyro3 are 270nM and 100nM, respectively. In addition, UNC2250 shows no significant inhibition of a panel of 30 other kinases. In cell-based assays, UNC2250 inhibits the phosphorylation of Mer with IC50 value of 9.8nM in B-ALL cells. It also prevents the colony formation both in BT-12 cell lines and in Colo699 NSCLC cell lines. Furthermore, UNC2250 is proved to have a moderate half-life, clearance, distribution volume and good oral bioavailability [1].

References:
[1] Zhang W, Zhang D, Stashko M A, et al. Pseudo-Cyclization through Intramolecular Hydrogen Bond Enables Discovery of Pyridine Substituted Pyrimidines as New Mer Kinase Inhibitors. Journal of medicinal chemistry, 2013, 56(23): 9683-9692.