Trametinib DMSO solvate

• CAT Number: I000673
• CAS Number: 1187431-43-1
• Molecular Formula: C28H29FIN5O5S
• Molecular Weight: 693.53
• Purity: ≥95%
• Synonyms: 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
• Target: MEK1/2
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.92 nM/1.8 nM (MEK1/2)
• 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 MEK1/2 inhibitor, used in cancer research to target the MAPK/ERK signaling pathway, which is critical for cell proliferation and survival. As a DMSO solvate, Trametinib’s solubility is enhanced, allowing for better formulation and administration in experimental settings. Trametinib is particularly effective in treating cancers with BRAF mutations, such as melanoma. By inhibiting MEK1/2, it prevents the activation of ERK, leading to reduced tumor cell growth. This compound is widely used to explore targeted therapies in oncology, especially in combination with other cancer treatments.

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.