Common name: Trametinib; GSK1120212; GSK-212; JTP-74057; GSK 1120212; Mekinist
Trademarks: Mekinist
Molecular Formula: C26H23FIN5O4
CAS Registry Number: 871700-17-3
CAS Name: N-(3-{3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)acetamide
Molecular Weight: 615.41
Activity: Oncolytic Drugs; Protein Kinase Inhibitor; Serine/Threonine-Protein Kinase B-raf Inhibitor; Serine/Threonine Inhibitor; MEK1 Inhibitor; MEK2 Inhibitor; MAP Kinase Inhibitor; MAP2K1 Inhibitor; MAP2K2 Inhibitor
Trametinib synthesis: US7378423
Trametinib synthesis: US7378423 (no intermediate separation needed)
References:
1. Kawasaki, H.; et al. Antiproliferative, anticancer, antitumor agents; rheumatism; N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-acetamide; a p15, and/or a protein inducing action, and/or an MEK inhibitory action; side effect reduction. US7378423
2. DeMarini, D. J.; et. al. Pharmaceutical composition. US8580304
3. Abe, H.; et. al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med Chem Lett 2011, 2(4), 320-324. (see suppl. for synthesis).
4. Waddell, J. A. and Solimando, Jr, D. A. Drug Monographs: Dabrafenib and Trametinib. Hosp Pharm 2013, 48(10), 818-821.
