Identification | Back Directory | [Name]
6,7-Dimethoxy-N-(4-phenoxyphenyl)- | [CAS]
179248-59-0 | [Synonyms]
Edr HB-1 Mar2 HHAT MART2 SKI-1 MEF3L Src I1 Src-l1 Src Inhibitor-1 Src Kinase Inhibitor 1 6,7-Dimethoxy-N-(4-phenoxyphenyl)- 46,7-Dimethoxy-N-(4-phenoxyphenyl)- Protein-cysteine N-palmitoyltransferase HHAT ANTI-HHAT (N-TERM) antibody produced in rabbit Monoclonal Anti-PEG10 antibody produced in mouse 6,7-Dimethoxy-N-(4-phenoxyphenyl)-aminoquinazoline 6,7-dimethoxy-N-(4-phenoxyphenyl)quinazolin-4-amine Src Kinase Inhibitor I - CAS 179248-59-0 - Calbiochem 4-Quinazolinamine, 6,7-dimethoxy-N-(4-phenoxyphenyl)- | [Molecular Formula]
C22H19N3O3 | [MDL Number]
MFCD01815300 | [MOL File]
179248-59-0.mol | [Molecular Weight]
373.4 |
Chemical Properties | Back Directory | [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. |
Hazard Information | Back Directory | [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 | [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 |
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