897016-82-9 5-[4-[2-(4-吗啉基)乙氧基]苯基]-N-(苯基甲基)-2-吡啶乙酰胺

KX2391
分子式：C26H29N3O3
分子量：431.53
产品描述
KX2-391 (KX01)是DY个临床SrcYZ剂(拟肽类)，处理癌细胞系，靶向作用于Src的肽底物位点, GI50为9-60 nM。
靶点
HuH7PLC/PRF/5Hep 3BHep G2 IC509 nM (GI50)13 nM (GI50)26 nM (GI50)60 nM (GI50)
体外研究
KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines.KX2-391 is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. KX2-391 is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively.
体内研究
In pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis.溶解性DMSO 86 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO