Trametinib, MEK inhibitor (TBI4759)

Description

Product Details

Formal Name: N-{3-[3-Cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide

Alternate Names: GSK1120212; JTP-74057

Molecular Formula: C₂₆H₂₃FIN₅O₄

Formula Weight: 615.40

CAS Number: 871700-17-3

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 20 mg/ml with warming)

Storage: -20°C

Stability: ≥ 1 year.

Applications

MEK inhibitor

Functions

Trametinib is a highly potent (IC50 uMEK1 = 0.7 nM, pp-MEK1 = 14.9 nM) and selective MEK inhibitor displaying selective inhibition of proliferation in various BRAF mutant cancer cell lines (IC50 ACHN = 9.8 nM; IC50 HT-29 = 0.57 nM). It is approved for use against unresectable or metastatic BRAF-mutant melanoma alone or in combination with Dabrafenib. Trametinib can limit outgrowth of tumors without directly inhibiting tumor cell proliferation via abrogation of cytokine-driven expansion of monocytic myeloid-derived suppressor cells (mMDSC) through a mechanism involving CD8+ T cells. Trametinib also displays potent anti-arthritic effects.

Application Procedures

First dissolved in DMSO (up to 20 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 2 months.