GLPBio

Src I1

Catalog No.: GC16957Purity:>99.50%
COASDSData Sheet
Src I1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

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Src I1
Cas No.: 179248-59-0
10mM (in 1mL DMSO)In Stock
$40.00
1
2mgIn Stock
$35.00
1
5mgIn Stock
$50.00
1
10mgIn Stock
$67.00
1
25mgIn Stock
$154.00
1
50mgIn Stock
$276.00
1
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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.

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].

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.

Protocol

Kinase experiment:

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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
179248-59-0
Chemical Name
6,7-dimethoxy-N-(4-phenoxyphenyl)quinazolin-4-amine
SMILES
COC(C=C1C(N=CN=C1NC(C=C2)=CC=C2OC3=CC=CC=C3)=C4)=C4OC
Molecular Formula
C22H19N3O3
Molecular Weight
373.4
Solubility
DMF: 0.25 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 2.5 mg/ml
Storage
Store at 2-8°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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