Trametinib (GSK1120212) , ≥98% , 871700-17-3

CAS NO.：871700-17-3

Empirical Formula: C26H23FIN5O4

Molecular Weight: 615.39

MDL number: MFCD17215075

PRODUCT Properties

• Melting point: 300-301 °C
• Density: 1.74
• storage temp.: -20°C
• solubility: Soluble in DMSO (up to 20 mg/ml)
• form: White solid.
• pka: 14.76±0.70(Predicted)
• color: White
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
• InChIKey: LIRYPHYGHXZJBZ-UHFFFAOYSA-N
• SMILES: C(NC1=CC=CC(N2C3=C(C)C(=O)N(C)C(NC4=CC=C(I)C=C4F)=C3C(=O)N(C3CC3)C2=O)=C1)(=O)C

Description and Uses

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 metastatic mutant B-RAF^V600E melanoma.

Used in the systematic treatment of advanced cutaneous melanoma. An EGFR kinase inhibitor and potent MEK inhibitor.

Safety

• Symbol(GHS): GHS08
• Signal word: Danger
• Hazard statements: H317-H361-H372
• Precautionary statements: P261-P272-P280-P302+P352-P333+P313-P321-P363-P501-P201-P202-P281-P308+P313-P405-P501-P260-P264-P270-P314-P501
• Safety Statements: 24/25
• HS Code: 29339900