6,7-Dimethoxy-N-(4-phenoxyphenyl)-

Description

Src-I1 (179248-59-0) is a potent and competitive dual site (ATP- and peptide-binding) Src kinase inhibitor (IC50‘s = 44 nM for Src and 88 nM for Lck). Src-I1 also inhibits VEGFR2 (IC50 = 320 nM).

Uses

Src Kinase inhibitor 1 lung cancers with EGF receptor abnormalities and is a potential candidate for mol.-targeted therapy

Uses

Src Inhibitor-1 may be used in Src kinase-mediated cell signaling studies.

Definition

ChEBI: Src Inhibitor-1 is a member of the class of quinazolines that is quinazoline which is substituted at position 4 by a p-phenoxyanilino group and at positions 6 and 7 by methoxy groups. It is a potent, competitive dual site (both the ATP- and peptide-binding) Src kinase inhibitor. Src Inhibitor-1 is one of the 'gold standards' for Src kinase inhibition that has been shown to use PP1 or PP2 in parallel with Src-I1 to inhbit Src family kinases. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor. It is a member of quinazolines, a secondary amino compound, an aromatic ether and a polyether.

General Description

A potent, selective, dual site, cell-permeable, reversible and ATP-competitive inhibitor of Src tyrosine kinase (IC₅₀ = 44 nM and 88 nM for Src and Lck, respectively). Shown to simultaneously interact with both the ATP- and peptide-binding sites. Inhibits VEGFR2 and c-fms tyrosine kinases only at higher concentrations (IC₅₀ = 320 nM and 30 μM, respectively).

Biochem/physiol Actions

Cell permeable: yes

storage

Desiccate at RT

References

1) Tian et al. (2001) Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines; Biochem. 40 7084 2) Bain et al. (2007) The selectivity of protein kinase inhibitors: a further update; Biochem. J. 408 297