4-[3-氯-4-(环丙基氨基羰基)氨基苯氧基]-7-甲氧基-6-喹啉甲酰胺

溶解度:DMSO

储存条件:-20℃ 2 years

生物活性

ABT-869 is multi-targeted in that it is a potent inhibitor of all members of the VEGF and PDGF receptor families (e.g., KDR IC50 value of 4 nM), but has much less activity (IC50 values >1 ) against unrelated receptor tyrosine kinases, soluble tyrosine kinases or serine/threonine kinases. The kinase inhibition profile of ABT-869 is evident in cellular assays of RTK phosphorylation (IC50 values of 2, 4 and 7 nM for PDGFR, KDR and CSF-1R, respectively) and VEGF-stimulated proliferation (0.2 nM IC50 for human endothelial cells).

参考文献

1, ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia. Shankar DB,et al Blood. 2007 Apr 15;109(8):3400-8.

2, Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Albert DH, Mol Cancer Ther. 2006 Apr;5(4):995-1006.