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    Purvalanol A (NG60)
    Purvalanol A (NG60)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1540
    CAS #: 212844-53-6Purity ≥98%

    Description: Purvalanol A is a potent and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. In MKN45 cells, purvalanol A (30 μM) reduced the expression of antiapoptotic proteins Bcl-2, Bcl-XL and survivin and induced apoptosis. Also, purvalanol A inhibited the phosphorylation of STAT3 by Janus kinase 2 (JAK2) and the expression and phosphorylation of RNA polymerase II, which was involved in transcriptional regulation.      

    References: Science. 1998;281(5376):533-8; Mol Biol Rep. 2014;41(1):145-54; Genes Cells. 2010;15(10):1051-62. 

    Related CAS: 212844-54-7 (Purvalanol B); 220792-57-4 (Aminopurvalanol A); 212844-53-6 (Purvalanol A)

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    Molecular Weight (MW)388.89
    FormulaC19H25ClN6O
    CAS No.212844-53-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 60 mg/mL (154.3 mM)
    Water: <1 mg/mL 
    Ethanol: 13 mg/mL (33.4 mM)
    Other info

    Chemical Name: (R)-2-((6-((3-chlorophenyl)amino)-9-isopropyl-9H-purin-2-yl)amino)-3-methylbutan-1-ol

    InChi Key: PMXCMJLOPOFPBT-HNNXBMFYSA-N

    InChi Code: InChI=1S/C19H25ClN6O/c1-11(2)15(9-27)23-19-24-17(22-14-7-5-6-13(20)8-14)16-18(25-19)26(10-21-16)12(3)4/h5-8,10-12,15,27H,9H2,1-4H3,(H2,22,23,24,25)/t15-/m0/s1

    SMILES Code: CC(C)[[email protected]@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO

    Synonyms

    NG60; NG-60; NG 60


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    In Vitro

    In vitro activity: Purvalanol A decreases cell viability in dose-dependent manner in MCF-7 and MDA-MB-231 cell lines. Purvalanol A induces cell viability loss by 50 % in MCF-7 cells but MDA-MB-231 cells sre less sensitive to Purvalanol A (32 % decreases in cell viability). Purvalanol A induces mitochondria-mediated apoptosis in MCF-7 and MDA-MB-231 cells. Purvalanol A effectively prevents c-Src-mediated transformation by inhibiting both cell cycle progression and c-Src signaling, and effectively suppresses the anchorage independent growth of some human cancer cells in which c-Src is up-regulated. Purvalanol A has a stronger inhibitory effect on the anchorage-independent growth of HT29 and SW480 human colon cancer cells.


    Kinase Assay: Purvalanol A is a potent CDK inhibitor, inhibiting cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.


    Cell Assay: Cells are seeded at 10000 density in 96-well plates and treated with various concentrations of Purvalanol A (0-100 μM) for 24 h. Cells are exposed to 10 μL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltet- razolium bromide dye (5 mg/mL) and are incubated at 37℃ for 4 h. In order to solubilize the formazan crystals 100 μL DMSO is added. Absorbance is determined at 570 nm spectrophotometrically.

    In VivoIn the dentate gyrus (DG) of the rat hippocampus, purvalanol A (40 nmol/3 μl) significantly induced the number of BrdU-positive cells in a time- and concentration-dependent way. 
    Animal modelRats
    Formulation & Dosage40 nmol/3 μl
    References

    Science. 1998 Jul 24;281(5376):533-8; Mol Biol Rep. 2014 Jan;41(1):145-54; Genes Cells. 2010 Oct;15(10):1051-62. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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