Description
A multi-kinase inhibitor; a pan inhibitor of FGFR (IC50s = 4.5, 1.8, 4.5, and 34 nM for FGFR1, -2, -3, and -4, respectively); inhibits 18 tyrosine kinases and the calcium/calmodulin-dependent protein kinase QIK in a panel of 297 kinases (IC50s = 3-31 and 9.7 nM, respectively); decreases phosphorylation of FGFR in COS-1 cells expressing FGFR1, -2, -3, or -4 (IC50s = 10 µM, respectively) and inhibits the growth of 15 cancer cell lines with mutant, amplified, or translocated FGFR (GI50s = 0.1-1.7 µM); reduces tumor growth and decreases tumor protein levels of phosphorylated FGFR, FRS2, and ERK in a SNU-16 mouse xenograft model at 50 and 75 mg/kg
Formal name: (6R)-6-(2-fluorophenyl)-5,6-dihydro-N-[3-[2-[(2-methoxyethyl)amino]ethyl]phenyl]-benzo[h]quinazolin-2-amine
Synonyms: ARQ 087
Molecular weight: 468.6
CAS: 1234356-69-4
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Kinase Inhibitors|CaMKs||Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling
