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BMS-599626 is a pan-HER inhibitor (including EGFR and VEGFR) that is currently in clinical trials as a potential treatment against several forms of cancer. BMS-599626 displays anticancer chemotherapeutic activity. In head and neck squamous cell carcinoma cells, BMS-599626 induces G1 phase cell cycle arrest and inhibits cell growth; in vivo, it improves responses to radiation.
| Cas No. | 714971-09-2 |
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| Purity | ≥98% |
| Formula | C27H27FN8O3 |
| Formula Wt. | 530.55 |
| IUPAC Name | [(3S)-morpholin-3-yl]methyl N-[4-[[1-[(3-fluorophenyl)methyl]indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamate |
| Synonym | BMS599626, AC480 |
| Solubility | DMSO 113 mg/mL (212.98 mM) Ethanol 20 mg/mL (37.69 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 |
Soria JC, Cortes J, Massard C, et al. Phase I safety, pharmacokinetic and pharmacodynamic trial of BMS-599626 (AC480), an oral pan-HER receptor tyrosine kinase inhibitor, in patients with advanced solid tumors. Ann Oncol. 2012 Feb;23(2):463-71. PMID: 21576284.
Torres MA, Raju U, Molkentine D, et al. AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Invest New Drugs. 2011 Aug;29(4):554-61. PMID: 20119866.