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RDEA119 inhibits MEK1/2 and exhibits anticancer chemotherapeutic activity. RDEA119 is currently in clinical trials as a potential treatment for a variety of advanced cancers. This compound inhibits proliferation in thyroid cancer cells, including those containing V600E B-Raf mutations. RDEA119 also inhibits tumor growth in animal models of melanoma, colon cancer, and epidermal carcinoma.
| Cas No. | 923032-37-5 |
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| Purity | ≥98% |
| Formula | C19H20F3lN2O5S |
| Formula Wt. | 572.34 |
| Chemical Name | Refametinib |
| IUPAC Name | N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide |
| Synonym | Refametinib, BAY 869766; N-[3,4-Difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]-cyclopropanesulfonamide; BAY 869766; BAY 8697661 |
| Solubility | DMSO 100 mg/mL (174.72 mM) Ethanol 100 mg/mL (174.72 mM) Water Insoluble |
| Appearance | White Powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet | |
| Brochures |
Weekes CD, Von Hoff DD, Adjei AA, et al. Multicenter phase I trial of the mitogen-activated protein kinase 1/2 inhibitor BAY 86-9766 in patients with advanced cancer. Clin Cancer Res. 2013 Mar 1;19(5):1232-43. PMID: 23434733.
Liu D, Xing J, Trink B, et al. BRAF mutation-selective inhibition of thyroid cancer cells by the novel MEK inhibitor RDEA119 and genetic-potentiated synergism with the mTOR inhibitor temsirolimus. Int J Cancer. 2010 Dec 15;127(12):2965-73. PMID: 21351275.
Iverson C, Larson G, Lai C, et al. RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Res. 2009 Sep 1;69(17):6839-47. PMID: 19706763.