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Trametinib is an inhibitor of MEK1 and -2. It inhibits B-RAF- and C-RAF-induced phosphorylation of MEK1 (IC50s = 3.4 and 1.8 nM, respectively) and MEK2 (IC50s = 1.6 and 0.92 nM, respectively). Trametinib inhibits the growth of two human colorectal cancer cell lines expressing mutant B-RAF (IC50s = 0.48 and 0.52 nM) and seven cell lines expressing mutant K-Ras (IC50s = 2.2-174 nM) but does not inhibit the growth of wild-type COLO 320DM cells expressing both B-RAF and K-Ras (IC50 = >10,000 nM). It reduces tumor growth in HT-29 and COLO 205 mouse xenograft models when used at doses of 0.3 and 1 mg/kg per day. Trametinib (0.03 and 0.1 mg/kg per day) also decreases M. tuberculosis-induced increases in hind paw volume in a rat model of arthritis. Formulations containing trametinib, in combination with dabrafenib, have been used in the treatment of metastatic mutant B-RAFV600E melanoma.Formal Name: N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-acetamide. CAS Number: 871700-17-3. Synonyms: GSK1120212, JTP-74057. Molecular Formula: C26H23FIN5O4. Formula Weight: 615.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 3 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 250, 330 nm. SMILES: CC(NC1=CC(N2C(C(C(N(C3CC3)C2=O)=O)=C(NC4=CC=C(I)C=C4F)N5C)=C(C)C5=O)=CC=C1)=O. InChi Code: InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34). InChi Key: LIRYPHYGHXZJBZ-UHFFFAOYSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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