468740-43-4

溶解度:DMSO

储存条件:at -20℃ 2 years

生物活性

BMS-536924 is a small molecule ATP-competitive IGF-IR kinase inhibitor with  with an IC50 of 80 nM. BMS-536924 also inhibits a small number of other kinases including insulin receptor. BMS-536924 inhibited this ligand-induced phosphorylation, consistent with the blockade of IGF-IR phosphorylation and activation. Basal levels of GSK3β and ERK1/2 phosphorylation were reduced by BMS-536924 potentially due either to low-level autocrine (IGF-I or IGF-II) activation of IGF-IR or due to BMS-536924 inhibition of other signaling pathways. Treatment of the IGF1R-Sal cells with BMS-536924 resulted in a dose-dependent inhibition of proliferation, with an IC50 of 0.11 nM. MCF7 cells were also significantly inhibited (IC50 = 0.46 nM). A different breast tumor cell line, BT474 was relatively insensitive to the compound, with an IC50 that is >10 fold higher than that for the IGF1R-Sal cells.

参考文献

[1] Jane Brokaw et al. Growth Factors.2007,25(5):346-354