| 货号 | 17708-1mg |
| 描述 | The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) promotes cell growth while inhibiting apoptotic pathways. Overexpression of IGF-1R is found in certain solid tumors and hematologic neoplasias.1,2 However, insulin receptor (InsR) signaling can compensate for IGF-1R inhibition.3 Linsitinib is a dual inhibitor of IGF-1R and InsR kinases (IC50s = 35 and 75 nM, respectively).4 It also inhibits InsR-related receptor (IC50 = 75 nM) but is without effect (IC50 > 10 µM) against a large panel of other kinases.4 Linsitinib inhibits proliferation of a variety of tumor cell lines in vitro and has antitumor efficacy in an IGF-1R-driven xenograft mouse model when administered orally.4 A rapid, non-invasive method to predict the pharmacodynamic response to linsitinib has been reported.3 |
| 别名 | OSI-906; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Scagliotti, G.V., and Novello, S. The role of the insulin-like growth factor signaling pathway in non-small cell lung cancer and other solid tumors. Cancer Treatment Reviews 38(4), 292-302 (2012). 2.McKinley, E.T.,Bugaj, J.E.,Zhao, P., et al. 18FDG-PET predicts pharmacodynamic response to OSI-906, a dual IGF-1R/IR inhibitor, in preclinical mouse models of lung cancer. Clinical Cancer Research 17(10), 3332-3340 (2011). 3.Buck, E.,Gokhale, P.C.,Koujak, S., et al. Compensatory insulin receptor (IR) activation on inhibition of insulin-like growth factor-1 receptor (IGF-1R): rationale for cotargeting IGF-1R and IR in cancer. Molecular Cancer Therapeutics 9(10), 2652-2664 (2010). 4.Mulvihill, M.J.,Cooke, A.,Rosenfeld-Franklin, M., et al. Discovery of OSI-906: A selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med.Chem. 1(6), 1153-1171 (2009). | |
| 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 | 421.5 |
| 分子式 | C26H23N5O |
| CAS号 | 867160-71-2 |
| 稳定性 | ≥ 2 years |
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