BMS-754807
Cat. No.：YN440055
CAS No. ：1001350-96-4
规格
价格(RMB)
库存
| 产品名称: | BMS-754807 |
| CAS No.: | 1001350-96-4 |
| Chemical Name: | 1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-(2S)-2-pyrrolidinecarboxamide |
| Synonyms: | BMS-754807;(2S)-1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide;BMS 754807;(2S)-1-[4-[(5-Cyclopropyl-1h-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-flu |
| 分子量: | 461.49 |
| 分子式: | C₂₃H₂₄FN₉O |
| SMILES: | FC1=CC=C(NC([C@@]2(C)N(C(N=C3NC4=NNC(C5CC5)=C4)=NN6C3=CC=C6)CCC2)=O)C=N1 |
| 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: | BMS-754807 是有效、可逆的IGF-1R/IR抑制剂，其IC50值分别为 1.8 和 1.7 nM，Ki值均小于 2 nM。BMS-754807 同时也抑制 Met，RON，TrkA，TrkB，AurA 和 AurB 的活性，IC50值分别为 6，44，7，4，9 和 25 nM。 |
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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 developmentJ. Med. Chem.52(23),7630-7363(2009)
Carboni, J.M., Wittman, M., Yang, Z., et al.BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IRMol. Cancer Ther.8(12),3341-3349(2009)
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 cancerMol. Cancer Ther.11(12),2644-2653(2012)
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 pathwaysPLoS One7(12),e51189(2012)
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 linesMol. Cancer Ther.14(2),620-630(2014)
