Src Inhibitor-1

Names

[ Name ]:
Src Inhibitor-1

[Synonym ]:
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

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]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src

Research Areas >> Cancer

[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.

[Related Small Molecules]

Saracatinib | PP2 (AG 1879) | A 419259 trihydrochloride | DCC-2036 (Rebastinib) | SU6656 | 1-Naphthyl PP1 | WH-4-023 | Pelitinib | ENMD-2076 | TC-S 7003 | PD173955 | TG 100572 (Hydrochloride) | XL228 | A-196 | pp1

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

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

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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