现货,BMS-536924,CAS号:468740-43-4,美国进口, 受体酪氨酸激酶(RTK), IGF-1R , IGF-1R 抑制剂和化合物,selleck,S1012

信号转导通路: 受体酪氨酸激酶(RTK) >> IGF-1R >> IGF-1R 抑制剂和化合物 >> BMS-536924http://www.dxy.cn/redirect?url=http://selleck.cn/bms-536924-S1012.html

技术数据:

分子量(MW): 479.96

化学式:

C25H26ClN5O3

 

溶解度:

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 468740-43-4

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. [1][2][3]

 

 

 

参考文献

IGF-I in epithelial ovarian cancer and its role in disease progression Brokaw J,et al. Growth Factors 2007;25:346–54

BMS-536924 sensitizes human epithelial ovarian cancer cells to the PARP inhibitor, 3-aminobenzamide Beauchamp MC,et al. Gynecologic Oncology 2009;193–198

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