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BMS-754807 is an inhibitor of the insulin receptor (InsR) and IGF-1R that exhibits anticancer chemotherapeutic activity. BMS-754807 enhances the efficacy of other co-administered chemotherapeutics, decreasing levels of activated Akt, increasing cleavage of PARP and caspase 3, and inhibiting proliferation in pancreatic ductal adenocarcinoma cells and breast cancer cells in vitro and growth of tumor xenografts in vivo.
| Cas No. | 1001350-96-4 |
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| Purity | ≥98% |
| Formula | C23H24FN9O |
| Formula Wt. | 461.51 |
| Chemical Name | (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 |
| IUPAC Name | (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 |
| Synonym | BMS754807; BMS 754807 |
| Solubility | DMSO 92 mg/mL (199.35 mM) Ethanol 92 mg/mL (199.35 mM) Water Insoluble |
| Appearance | White to off white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
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. Mol Cancer Ther. 2012 Dec;11(12):2644-53. PMID: 23047891.
Hou X, Huang F, Macedo LF, et al. Dual IGF-1R/InsR inhibitor BMS-754807 synergizes with hormonal agents in treatment of estrogen-dependent breast cancer. Cancer Res. 2011 Dec 15;71(24):7597-607. PMID: 22042792.