Trametinib-13C-d3

Trametinib-13C-d3 is intended for use as an internal standard for the quantification of trametinib (Cay-16292) by GC- or LC-MS. 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 B-RAFV600E mutant metastatic melanoma.Formal Name: N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6-methyl-8-(methyl-13C-d3)-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-acetamide. CAS Number: 2712126-59-3. Molecular Formula: C25[13C]H20D3FIN5O4. Formula Weight: 619.4. Purity: >99% deuterated forms (d1-d3). Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: CC(NC1=CC(N2C(C(C(N(C3CC3)C2=O)=O)=C(NC4=CC=C(I)C=C4F)N5C)=C([13C]([2H])([2H])[2H])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)/i1+1D3. InChi Key: LIRYPHYGHXZJBZ-KQORAOOSSA-N.