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GSK-1120212 inhibits MEK1/2 and is currently in clinical trials as a potential treatment for melanoma. GSK-1120212 exhibits anticancer chemotherapeutic activity, upregulating p27 expression and inhibiting growth in colorectal cancer cells and suppressing tumor growth in colorectal cancer xenografts.
| Cas No. | 871700-17-3 |
|---|---|
| Purity | ≥98% |
| Formula | C26H23FlN5O4 |
| Formula Wt. | 615.39 |
| IUPAC Name | N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide |
| Synonym | Trametinib, JTP-74057 |
| Solubility | DMSO (10 mg/ml) Water Insoluble Ethanol Insoluble |
| Appearance | White Powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet | |
| Brochures |
Hartsough EJ, Basile K, Aplin AE. Beneficial Effects of RAF Inhibitor in Mutant BRAF Splice Variant-expressing Melanoma. Mol Cancer Res. 2014 Feb 11. [Epub ahead of print]. PMID: 24520098.
Kim KB, Kefford R, Pavlick AC, et al. Phase II study of the MEK1/MEK2 inhibitor Trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitor. J Clin Oncol. 2013 Feb 1;31(4):482-9. PMID: 23248257.
Yamaguchi T, Kakefuda R, Tajima N, et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol. 2011 Jul;39(1):23-31. PMID: 21523318.