General description
一种新型的高效的可口服利用的Mer/FLT3双抑制剂，IC50分别为0.74nM和0.8nM。
UNC2025 is a novel potent and highly orally bioavailable Mer/FLT3 dual inhibitor, capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC-2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined。
UNC2025是一种新型的有效且高度口服生物利用的Mer / FLT3双重抑制剂，在口服给药后能够抑制体内的Mer磷酸化，如药效学（PD）研究通过检测小鼠骨髓白血病细胞中的磷酸化Mer所证实的那样。 激酶组分析与300多种激酶的体外和细胞选择性评估表明，UNC-2025具有对抗Flt3的亚纳摩尔活性，Flt3是急性骨髓性白血病（AML）的另一个重要目标，其药理学选择性优于其他激酶。
Properties
| Inchi Code： | 1S/C28H40N6O.2ClH/c1-3-4-13-29-28-30-18-25-26(20-34(27(25)31-28)23-9-11-24(35)12-10-23)22-7-5-21(6-8-22)19-33-16-14-32(2)15-17-33;;/h5-8,18,20,23-24,35H,3-4,9-17,19H2,1-2H3,(H,29,30,31);2*1H/t23-,24-;; |
| Inchi Key | GAZBHOHQEDSYPG-PZPNUJOOSA-N |
安全信息
