Description
A multi-kinase inhibitor; inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 252, 15, 6, 15, and 3 nM, respectively); only inhibits RAFs, Src, LCK, and MAPKs in a panel of 63 kinases at 1 µM; inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells; inhibits growth of B-RAF mutant melanoma cells; induces tumor regression in a B-RAF mutant A375 mouse xenograft model at 20 mg/kg per day; inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant PDX mouse models
Formal name: N-[4-[(3,4-dihydro-3-oxopyrido[2,3-b]pyrazin-8-yl)oxy]-2-(methylthio)phenyl]-N’-[3-(1,1-dimethylethyl)-1-phenyl-1H-pyrazol-5-yl]-urea
Synonyms:
Molecular weight: 541.6
CAS: 1163719-91-2
Purity: ≥98%
Formulation: A solid
Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Cancer|Cell Signaling|SRC Family Signaling
