PP2 - CAS 172889-27-9

Catalog Number Size Price Stock Quantity
BP-300123 100 mg $439 In stock
BP-300123 1 g $943 In stock
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PP2 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. It inhibits p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM), and Src (IC50 = 100 nM).

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Molecular Formula
C15H16ClN5
Molecular Weight
301.77

PP2

    • Specification
      • IUPAC Name
        1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine
        Synonyms
        PP-2; PP 2; AG 1879; AG-1879; AG1879
    • Properties
      • InChI Key
        PBBRWFOVCUAONR-UHFFFAOYSA-N
        InChI
        InChI=1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)
        Canonical SMILES
        CC(C)(C)N1C2=C(C(=N1)C3=CC=C(C=C3)Cl)C(=NC=N2)N
    • Reference Reading
      • 1.Src kinase family inhibitor PP2 induces aggregation and detachment of neuroblastoma cells and inhibits cell growth in a PI3 kinase/Akt pathway-independent manner
        Tomoro Hishiki • Takeshi Saito • Yoshiharu Sato • Tetsuya Mitsunaga. Pediatr Surg Int (2011) 27:225–230
        To study the role of src kinase families in NB, we first studied the morphological response of NB cell lines to src family inhibitor PP2 treatment. NB cell lines (SH-SY5Y, IMR32, RT-BM-1, CHP134, NLF, LA-N-5) were cultured in 0.1, 1, and 10 lM of PP2. Representative results are shown in Fig. 1a. All cell lines showed morphological changes by becoming round-shaped and forming aggregated cell clusters. Particularly, IMR32 and RT-BM-1 cells showed drastic clustering followed by detachment of cells from the culture dish. The majority of the floating cells were however viable, as shown by Trypan blue assay (data not shown). These changes occurred as early as 3 h after treatment with 10 lM of PP2. Contrastly, human fibroblast cells did not show significant change after PP2 treatment, suggesting that the inhibition of src family kinases has minimum effect on non-transformed cells.
        2.Src family kinase inhibitor PP2 efficiently inhibits cervical cancer cell proliferation through down-regulating phospho-Src-Y416 and phospho-EGFR-Y1173
        Lu Kong • Zhihong Deng • Haiying Shen • Yuxiang Zhang. Mol Cell Biochem (2011) 348:11–19
        Recently, the results of a large body of preclinical studies and clinical trials suggest that targeting the EGFR could represent a significant contribution to cancer therapy. Tyrosine kinases show promise as new therapeutic targets, and a number of tyrosine kinase inhibitors are currently undergoing clinical evaluation as cancer therapies. However, relatively little is known regarding these targeting on cervical cancer. In this paper, we presented evidence that PP1, PP2, and PP3 targeted different tyrosine phosphorylation sites on EGFR and Src, which may help to explain their different efficacies on inhibition of cervical cancer cell proliferation.
    • Preparing Stock Solutions
      • ConcentrationVolumeMass1 mg5 mg10 mg
        1 mM3.3138 mL16.5689 mL33.1378 mL
        5 mM0.6628 mL3.3138 mL6.6276 mL
        10 mM0.3314 mL1.6569 mL3.3138 mL
        50 mM0.0663 mL0.3314 mL0.6628 mL
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