| 货号 | 14666-25mg |
| 描述 | BMS-536924 is a dual inhibitor of insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IC50s = 100 and 73 nM, respectively).1 In this way, it blocks IGF-1R autophosphorylation and signaling through MEK1/2 and Akt, leading to G1 arrest and apoptosis in myeloblastic leukemia ML-1 cells. BMS-536924 reverses epithelial-to-mesenchymal transition in immortalized mammary epithelial MCF10A cells overexpressing constitutively activated IGF-1R and causes growth inhibition and polarization of breast cancer MCF-7 cells.2,3 It also induces expression of cytochrome P450 3A4 isoform in primary hepatocytes.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Wittman, M.,Carboni, J.,Attar, R., et al. Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. Journal of Medicinal Chemistry 48(18), 5639-5643 (2005). 2.Kim, H.J.,Litzenburger, B.C.,Cui, X., et al. Constitutively active type I insulin-like growth factor receptor causes transformation and xenograft growth of immortalized mammary epithelial cells and is acompanied by an epithelial-to-mesenchymal transition mediated by NF-κB and snail. Mol.Cell Biol. 27(8), 3165-3175 (2007). 3.Litzenburger, B.C.,Kim, H.J.,Kuiatse, I., et al. BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cells. Clinical Cancer Research 15(1), 226-237 (2009). 4.Li, L.,Sinz, M.W.,Zimmermann, K., et al. An insulin-like growth factor 1 receptor inhibitor induces CYP3A4 expression through a pregnane X receptor-independent, noncanonical constitutive androstane receptor-related mechanism. Journal of Pharmacology and Experimental Therapeutics 340(3), 688-697 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 480 |
| 分子式 | C25H26ClN5O3 |
| CAS号 | 468740-43-4 |
| 稳定性 | ≥ 2 years |
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