Description
An inhibitor of Raf kinases (Kis = 0.3, 1, and 1 nM for C-RAF, B-RAF, and B-RAFV600E, respectively); selective for B-RAFV600E kinase domain over Lck, Tie2, KDR, and p38α (IC50s = 83, 120, 1,000, and >1,600 nM, respectively); inhibits phosphorylation of ERK in A375 melanoma cells (IC50 = 1.8 nM); reduces tumor growth in an A375 SQ2 mouse xenograft model (ED50 = 1.3 mg/kg per day) and induces 85% tumor regression at 5 mg/kg per day for 14 days; increases tumor growth in a MIA PaCa-2 mouse xenograft model at 5 and 10 mg/kg per day
Formal name: N1-(4-chlorophenyl)-6-methyl-N5-[3-(9H-purin-6-yl)-2-pyridinyl]-1,5-isoquinolinediamine, dihydrochloride
Synonyms:
Molecular weight: 551.9
CAS: 1191385-19-9
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling
