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Src kinase inhibitor I

  Cat. No.:  DC9992   Featured
Chemical Structure
179248-59-0
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More than 5000 active chemicals with high quality for research!
Field of application
Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 179248-59-0
Chemical Name: 6,7-dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine
Synonyms: Src I1
SMILES: COC1=C(OC)C=C(N=CN=C2NC3=CC=C(OC4=CC=CC=C4)C=C3)C2=C1
Formula: C22H19N3O3
M.Wt: 373.4
Purity: >98%
Sotrage: 4°C for 1 year, -20°C for more than 2 years
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.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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