| 货号 | 17505-1mg |
| 描述 | BMS 754807 is a reversible, orally bioavailable dual inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases (IC50s = 1.8 and 1.7 nM, respectively).1,2 It has minimal effect against an array of other tyrosine and serine/threonine kinases.1 BMS 754807 inhibits cell proliferation or induces apoptosis in a variety of cancer cells in vitro.2 It inhibits the growth of tumor xenografts in mice and this effect is often enhanced by combination therapy with other chemotherapeutics.2,3,4 Predictive biomarkers, including elevated IGF-1R expression, for effectiveness of BMS 754807 have been delineated.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Wittman, M.D.,Carboni, J.M.,Yang, Z., et al. Discovery of a 2,4-disubstituted pyrrolo-[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development. Journal of Medicinal Chemistry 52, 7630-7363 (2009). 2.Carboni, J.M.,Wittman, M.,Yang, Z., et al. BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR. Molecular Cancer Therapeutics 8(12), 3341-3349 (2009). 3.Awasthi, N.,Zhang, C.,Ruan, W., et al. BMS-754807, a small-molecule inhibitor of insulin-like growth factor-1 receptor/insulin receptor, enhances gemcitabine response in pancreatic cancer. Molecular Cancer Therapeutics 11(12), 2644-2653 (2012). 4.Dayyani, F.,Parikh, N.U.,Varkaris, A.S., et al. Combined inhibition of IGF-1R/IR and Src family kinases enhances antitumor effects in prostate cancer by decreasing activated survival pathways. PLoS One 7(12), 1-10 (2012). 5.Huang, F.,Chang, H.,Greer, A., et al. IRS2 copy number gain, KRAS and BRAF mutation status as predictive biomarkers for response to the IGF-1R/IR inhibitor BMS-754807 in colorectal cancer cell lines. Molecular Cancer Therapeutics 14(2), 620-630 (2014). | |
| 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 | 461.5 |
| 分子式 | C23H24FN9O |
| CAS号 | 1001350-96-4 |
| 稳定性 | ≥ 2 years |
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