AV-412/AV412

Solubility:Soluble to 5 mM in DMSO

Storage:Desiccate at -20°C

Biologieal

Potent and selective inhibitor of epidermal growth factor receptor kinase (IC50 values 3 nM for EGFR and > 100 ��M for ErbB2 and PDGFR). Inhibits proliferation of NCI-H2170 NSCLC cells in vitro (IC50 = 1 ��M).

Reference

Levitzki and Gazit (1995) Tyrosine kinase inhibition: an approach to drug development. Science 267 1783. Han et al (1996) Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors. Cancer Res. 56 3859. Eguchi et al (1998) Calcium-dependent epidermal growth factor receptor transactivation mediates the angiotensin II-induced mitogen-activated protein kinase activation in vascular smooth muscle cells. J.Biol.Chem. 273 8890. Puri and Salgia (2008) Synergism of EGFR and c-Met pathways, cross-talk and inhibition, in non-small cell lung cancer. J.Carcinog. 7 9.