Description
An inhibitor of MEK1 and -2; 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); 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); reduces tumor growth in HT-29 and COLO 205 mouse xenograft models at 0.3 and 1 mg/kg per day; decreases M. tuberculosis-induced increases in hind paw volume in a rat model of arthritis at 0.03 and 0.1 mg/kg per day
Formal name: N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-acetamide
Synonyms: GSK1120212|JTP-74057
Molecular weight: 615.4
CAS: 871700-17-3
Purity: ≥95%
Formulation: A crystalline solid
Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis
