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    UM-164
    UM-164

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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 #: V3287
    CAS #: 903564-48-7 Purity ≥98%

    Description: UM-164, a dasatinib analogue, is a potent and dual inhibitor of the Src/p38 kinase with potential anticancer activity for Triple-Negative Breast Cancer (TNBC). It is a promising lead compound for developing the first targeted therapeutic strategy against TNBC. c-Src has been shown to play a pivotal role in breast cancer progression, metastasis, and angiogenesis. In the clinic, however, the limited efficacy and high toxicity of existing c-Src inhibitors have tempered the enthusiasm for targeting c-Src. UM-164 binds the inactive kinase conformation of c-Src. Kinome-wide profiling of UM-164 identified that Src and p38 kinase families were potently inhibited by UM-164. UM-164 alters the cell localization of c-Src in TNBC cells. In xenograft models of TNBC, UM-164 resulted in a significant decrease of tumor growth compared with controls, with limited in vivo toxicity. 

    References:  2018 Jul;185(3):655-675;  2016 Oct 15;22(20):5087-5096;  2017 May 30;13(6):1157-1171. 


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    Molecular Weight (MW) 640.69
    Formula C30H31F3N8O3S
    CAS No. 903564-48-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10mM
    Water: 
    Ethanol: 
    Chemical Name 2-[[6-[4-(2-Hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide
    Synonyms UM-164; UM 164; UM164
    SMILES Code O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCO)CC3)=C2)S1)NC4=CC(NC(C5=CC=CC(C(F)(F)F)=C5)=O) =CC=C4C



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    In Vitro

    In vitro activity: UM-164 is a potent Src/p38 inhibitor with potential anticancer activity for Triple-Negative Breast Cancer (TNBC). It is a promising lead compound for developing the first targeted therapeutic strategy against TNBC. c-Src has been shown to play a pivotal role in breast cancer progression, metastasis, and angiogenesis. In the clinic, however, the limited efficacy and high toxicity of existing c-Src inhibitors have tempered the enthusiasm for targeting c-Src. UM-164 binds the inactive kinase conformation of c-Src. Kinome-wide profiling of UM-164 identified that Src and p38 kinase families were potently inhibited by UM-164. UM-164 alters the cell localization of c-Src in TNBC cells. In xenograft models of TNBC, UM-164 resulted in a significant decrease of tumor growth compared with controls, with limited in vivo toxicity. 


    Kinase Assay: UM-164 is a potent and dual inhibitor of the Src/p38 kinase with potential anticancer activity. UM-164 binds the inactive kinase conformation of c-Src. Kinome-wide profiling of UM-164 identified that Src and p38 kinase families were potently inhibited by UM-164. 


    Cell Assay: MDA-MB 468 cells were trypsinized and allowed to adhere overnight to #1.5 cover glass in a 6-well plate. Cells were then treated with 5 μmol/L dasatinib, 5 μmol/L UM-164, or vehicle (DMSO) for 4 hours. Cells were then fixed with 4% paraformaldehyde for 15 minutes at room temperature followed by three washes with PBS. The fixed cells were treated with 1 μmol/L of an irreversible turn-on Src fluorophore for 1 hour followed by three washes with PBS. Cells were then mounted on slides with UltraCruz Hard-set Mounting Medium w/DAPI (Santa Cruz Biotechnology; sc-359850) and stored for 30 minutes at 4°C in the dark. 

    In VivoIn xenograft models of TNBC, UM-164 resulted in a significant decrease of tumor growth compared with controls, with limited in vivo toxicity. 
    Animal model NCr/nude mice, 6 weeks of age
    Formulation & Dosage Dissolved in a mixture of DMSO/propylene glycol (1:9); 10 mg/kg, 15 mg/kg, or 20 mg/kg; i.p. injection
    References  2018 Jul;185(3):655-675;  2016 Oct 15;22(20):5087-5096;  2017 May 30;13(6):1157-1171. 


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

    UM-164

    Chemical structures of dasatinib and UM-164. A, UM-164 is a dasatinib analogue with an appended trifluoromethyl amide group (colored red) that causes binding to the inactive conformation of c-Src. B and C, MDA-MB 231 and SUM 149 cells were treated with UM-164 for 15, 30, 60, and 120 minutes at the indicated concentrations, and the whole-cell lysate was probed for P-Src/Tyr-419.  2016 Oct 15;22(20):5087-5096.

    UM-164

    Inhibition of multiple signaling pathways by UM-164 and dasatinib in TNBC cell lines. Cells were treated with an increasing concentration of either UM-164 or dasatinib for 1 hour. Whole-cell lysates were collected and analyzed for the phospho-specific antibody of the indicated proteins, followed by immunoblotting for the corresponding total protein. A, SUM 149. B, MDA-MB 231. C, VARI-068, a TNBC cell line grown from a PDX.  2016 Oct 15;22(20):5087-5096.

    UM-164

    Altered localization of c-Src when bound by UM-164. Representative fluorescence microscopy images of MDA-MB 468 cells treated with vehicle (DMSO), 5 μmol/L dasatinib, or 5 μmol/L UM-164 for 4 hours. In the vehicle-treated cells, c-Src (green) is predominately localized to the cell membranes. UM-164–treated cells show cytoplasmic punctate structures indicated by the white triangles. Nuclei are stained in blue (DAPI). Scale bar, 20 μm.  2016 Oct 15;22(20):5087-5096.

    UM-164

    UM-164 treatment inhibits cell motility and invasion through c-Src–mediated FAK activation.  2016 Oct 15;22(20):5087-5096.

    UM-164

    MDA-MB 231 and SUM 149 xenograft models.  2016 Oct 15;22(20):5087-5096.



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