FAK inhibitor 14
FAK inhibitor / Selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. Prevents FAK autophosphorylation at Y397 (IC50 = 1 μM), promotes cell detachment and inhibits cell adhesion in vitro. Exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo. Induces regression of pancreatic tumors2 and glioblastoma3. Displays antiangiogenic activity4.
Biochemicals & reagents
4506-66-5
Y15
1) Golubovskaya et al. (2008), A small mo;ecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the y397 site of focal adhesion kinase decreases tumor growth; J. Med. Chem., 51 7405 2) Hochwald et al. (2009), A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer; Cell Cycle, 8 2435 3) Golubovskaya et al. (2013), Pharmacologic blockade of FAK autophosphorylation decreases human glioblastoma tumor growth and synergizes with temozolomide; Mol. Cancer Ther., 12 162 4) Cabrita et al. (2011), Focal Adhesion kinase inhibitors are potent anti-angiogenic agents; Mol. Oncol., 5 517
-20°C
TARGET: Kinase -- PATHWAY: Cell adhesion; Proliferation -- RESEARCH AREA: Angiogenesis -- DISEASE AREA: Cancer