Trametinib DMSO solvate

• CAT Number: I000673
• CAS Number: 1187431-43-1
• Molecular Formula: C28H29FIN5O5S
• Molecular Weight: 693.53
• Purity: ≥95%
• Target: MEK1/2
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.92 nM/1.8 nM (MEK1/2) [1]
• 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;methylsulfinylmethane
• InChI: InChI=1S/C26H23FIN5O4.C2H6OS/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;1-4(2)3/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34);1-2H3
• InChIKey: OQUFJVRYDFIQBW-UHFFFAOYSA-N
• SMILES: CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC=CC(=C4)NC(=O)C)C5CC5.CS(=O)C

Trametinib DMSO solvate (Cat.No:I000673) is a pharmaceutical compound used as a selective inhibitor of mitogen-activated protein kinase (MAPK) kinase (MEK). It is approved for the treatment of certain types of advanced or metastatic cancers with BRAF V600E or V600K mutations. Trametinib DMSO solvate has demonstrated significant efficacy in clinical trials and offers a targeted approach in cancer therapy.

Reference

[1]. Yamaguchi T, 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, 39(1), 23-31.
[2]. Yamaguchi T, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with leflunomide. Inflamm Res, 2012, 61(5), 445-454.
[3]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20.