Linsitinib
Cat. No.:YN440050
产品名称: | Linsitinib |
CAS No.: | 867160-71-2 |
Chemical Name: | cis-3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol |
Synonyms: | OSI-906 |
分子量: | 421.49 |
分子式: | C₂₆H₂₃N₅O |
SMILES: | O[C@@]1(C)C[C@@H](C2=NC(C3=CC=C4C=CC(C5=CC=CC=C5)=NC4=C3)=C6C(N)=NC=CN62)C1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Linsitinib (OSI-906) 是一种有效选择性的,具有口服活性的IGF-1和胰岛素受体(IR)的双重抑制剂,IC50分别为 35 和 75 nM。 |
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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 tumorsCancer Treat. Rev.38(4),292-302(2012)
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 cancerClin. Cancer Res.17(10),3332-3340(2011)
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 cancerMol. Cancer Ther.9(10),2652-2664(2010)
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 receptorFuture Med. Chem.1(6),1153-1171(2009)