Trametinib, DMSO Solvate (GSK-1120212, JTP-74057, Mekinist, CAS 1187431-43-1), 99%

LC Laboratories' Product Number T-8188 - Trametinib, DMSO Solvate (GSK-1120212, JTP-74057, Mekinist, CAS 1187431-43-1), 99% - for research use only. Trametinib is a selective MEK inhibitor. Trametinib inhibited MEK1/2 kinase activity, prevented Raf-dependent MEK phosphorylation, and produced prolonged p-ERK1/2 inhibition. It blocked the cell growth potently in most tumor lines with mutant BRAF or Ras. In xenograft tumor models, trametinib inhibited tumor growth, possibly by sustained suppression of p-ERK1/2, inhibition of tumor Ki67, and stimulation of p27Kip1/CDKN1B. The largest antitumor effect in vivo was among tumors harboring mutant BRAF or Ras. A phase 1 clinical trial demonstrated substantial clinical activity of trametinib in human melanoma. Trametinib improved rates of progression-free and overall survival among patients who had metastatic melanoma with a BRAF V600E or V600K mutation when compared with dacarbazine or paclitaxel. Both trametinib and leflunomide can suppress adjuvant-induced arthritis (AIA) and type II collagen-induced arthritis (CIA) development completely. In the CIA model, trametinib, but not leflunomide, inhibited collagen-reactive T-cell proliferation ex vivo, whereas leflunomide, but not trametinib, inhibited anti-collagen antibody production. For solid tumors, RAF/RAS mutation and the expression of the DUSP6 gene were strong predictors of sensitivity to trametinib. Among hematologic cell lines, acute and chronic myeloid leukemia cell lines were particularly sensitive to trametinib. Trametinib had favorable antitumor activities against colorectal cancers in vitro and in vivo. It exhibited an additive or a synergistic effect in combination with other chemotherapy agents including 5-fluorouracil, oxaliplatin, or SN-38. Related CAS number: 1187431-43-1 for the dimethylsulfoxide solvate of trametinib. Another CAS number previously assigned to Trametinib, namely 1204531-14-5, has been deleted by CAS and is no longer in use.

• Supplier: LC Laboratories
• Product #: T-8188
• Sku #: T-8188_100mg