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

storage temp. 

2-8°C

solubility 

DMSO: >10mg/mL

form 

white powder

color 

White or off-white

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 week.

Safety

Hazard Codes 

Xn

Risk Statements 

22-36/37/38

Safety Statements 

26

RIDADR 

UN 3077 9 / PGIII

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P337+P313IF eye irritation persists: Get medical advice/attention.

P405Store locked up.

6,7-Dimethoxy-N-(4-phenoxyphenyl)- Chemical Properties,Usage,Production

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