KW-2449

属性

溶解性	DMSO 67 mg/mL Water <1 mg/mL Ethanol 67 mg/mL
存贮条件	储存温度-20°C

描述

应用	A multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase。
产品介绍	KW-2449能较强地抑制Flt3，IC50为6.6 nM，对FGFR1，Bcr-Abl和Aurora A的抑制性适中，而对 PDGFRβ，IGF-1R，EGFR则无抑制性。
生化机理	KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase. KW 2449 displays potent inhibition of growth effects on leukemia cells with FLT3 mutations via inhibition of the FLT3 kinase, resulting in the down-regulation of phosphorylated-FLT3/STAT5, G1 arrest, and apoptosis. KW 2449 induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis in FLT3 wild-type human leukemia. KW 2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases in imatinib-resistant leukemia.
别名	KW 2449; KW2449；[4-[2-(1H-吲唑-3-基)乙烯基]苯基]-1-哌嗪基甲酮;KW 2449;KW2449；[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone