MEK/ERK pathway inhibitor; Inhibits B-RAF, B-RAFV600E, and C-RAF-1
CAS
878739-06-1
Quantité
1 mg
Formule moléculaire
C27H25N5O2
Pureté
≥98%
Marque
STEMCELL Technologies
Caractéristiques principales
AZ628 is a quinazolinone that inhibits several Rapidly accelerated fibrosarcoma (RAF) kinases, including B-RAF, B-RAF V600E, and C-RAF-1 (in vitro kinase assay IC50 values of 105, 34, and 29 nM respectively; Khazak et al.) It strongly promotes B-Raf dimerization as a tight-binding inhibitor with a very slow off rate (Hatzivassiliou et al.; Lavoie et al.) From specificity profiling it is known to prevent activation of several other tyrosine kinases, including kinase insert domain receptor (KDR), discoidin domain receptor 2 (DDR2), Lck/Yes Novel (LYN), feline McDonough sarcoma (FMS), and FMS-like tyrosine kinase 1 (FLT1) (Khazak et al.)
Inhibits tumor growth, induces cell cycle arrest and causes apoptosis in a variety of cancer cell lines, especially in lines with the B-RAF V600E mutation (McDermott et al.; Khazak et al.)
