Src Inhibitor-1

Modify Date: 2024-01-02 18:44:00

Src Inhibitor-1 Structure
Src Inhibitor-1 structure
Common Name Src Inhibitor-1
CAS Number 179248-59-0 Molecular Weight 373.405
Density 1.3±0.1 g/cm3 Boiling Point 528.2±50.0 °C at 760 mmHg
Molecular Formula C22H19N3O3 Melting Point N/A
MSDS Chinese USA Flash Point 273.2±30.1 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of Src Inhibitor-1


Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

 Names

Name 6,7-dimethoxy-N-(4-phenoxyphenyl)quinazolin-4-amine
Synonym More Synonyms

 Src Inhibitor-1 Biological Activity

Description Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
Related Catalog
Target

IC50: 44 nM (Src), 88 nM (Lck)[1]

In Vitro Src-I1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[1]. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[2].
Kinase Assay Assays (25.5 μL volume) are carried out robotically at room temperature (21°C) and are linear with respect to time and enzyme concentration under the conditions used. Assays are performed for 30 min using Multidrop Micro reagent dispensers in a 96-well format. The concentration of magnesium acetate in the assays is 10 mM and [γ-33P]ATP (800 c.p.m./pmol) is used at 5, 20 or 50 μM as indicated, in order to be at or below the Kmfor ATP for each enzyme.The assays are initiated with MgATP, stopped by the addition of 5 μL of 0.5 M orthophosphoric acid and spotted on to P81 filter plates using a unifilter harvester. The IC50 values of inhibitors are determined after carrying out assays at ten different concentrations of each compound[2].
References

[1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.

[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 528.2±50.0 °C at 760 mmHg
Molecular Formula C22H19N3O3
Molecular Weight 373.405
Flash Point 273.2±30.1 °C
Exact Mass 373.142639
PSA 65.50000
LogP 4.90
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.665
Storage condition 2-8°C

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H315-H319-H335-H413
Precautionary Statements P280-P301 + P312 + P330-P305 + P351 + P338-P337 + P313
RIDADR UN 3077 9 / PGIII

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 Synonyms

6,7-Dimethoxy-N-(4-phenoxyphenyl)quinazolin-4-amine
Src Kinase Inhikitor
Src Kinase Inhibitor I
6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine
Src-l1
4-Quinazolinamine, 6,7-dimethoxy-N-(4-phenoxyphenyl)-
Src Inhibitor-1
KIN001-030
Src Inhibitor 1
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