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    Tasquinimod (ABR-215050; TASQ)
    Tasquinimod (ABR-215050; TASQ)

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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 #: V0268
    CAS #: 254964-60-8Purity ≥98%

    Description: Tasquinimod (also known as ABR215050), a quinoline-3-carboxamide linomide analogue and an investigational drug, is a novel, and orally bioactive anti-angiogenic agent which potently inhibits HDAC4 allosterically with with potential anticancer activity. Tasquinimod is currently being studied in Phase 3 clinical trials for the treatment of castration-resistant prostate cancer.

    References: Cancer Res. 2013 Feb 15;73(4):1386-99; Prostate. 2006 Dec 1;66(16):1768-78; Cancer Chemother Pharmacol. 2014 Jan;73(1):1-8. 

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    Molecular Weight (MW)406.36
    FormulaC20H17F3N2O
    CAS No.254964-60-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 81 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: 11 mg/mL warmed (27.1 mM)
    Solubility (In vivo)5% DMSO+30% PEG 300+ddH2O: 8 mg/mL
    Synonyms

    ABR-215050; ABR215050; ABR 215050; 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-((4-trifluoromethyl)phenyl)-1,2-dihydroquinoline-3-carboxamide

    InChi Key: ONDYALNGTUAJDX-UHFFFAOYSA-N

    InChi Code: InChI=1S/C20H17F3N2O4/c1-24(12-9-7-11(8-10-12)20(21,22)23)18(27)16-17(26)15-13(25(2)19(16)28)5-4-6-14(15)29-3/h4-10,26H,1-3H3

    SMILES Code: O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2OC)N(C)C3=CC=C(C(F)(F)F)C=C3


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    In Vitro

    In vitro activity: Tasquinimod inhibits tumor angiogenesis by allosteric inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α. Tasquinimod also targets infiltrating myeloid cells, and modulates local tumour immunity by blocking the interaction between S100A9 and its ligands receptor of advanced glycation end products and Toll-like receptor 4.


    Kinase Assay:  Tasquinimod binds to the regulatory Zn2+ binding domain of HDAC4 with Kd of 10-30 nM.


    Cell Assay: Generated microarray data based on four separate biological replicates showed a drug-induced effect of 50μM tasquinimod on gene expression in LNCaP cells when cultured in vitro for 24 h. The expression data achieved by RT-PCR were consistent with the microarray analysis data with a significant up-regulation of THBS1, GDF15 and CYP1A1 whereas CXCR4 and AGER1 did not change expression significantly.

    In VivoTasquinimod (30 mg/kg/d p.o.) shows anti-angiogenic activity and thus causes tumor growth inhibition in mice bearing human and rodent prostate cancer models.
    Animal modelMice bearing PC-82 , CWR-22Rv1, LAPC-4, or LNCaP prostate cancer xenografts.
    Formulation & DosageDissovled in water; 30 mg/kg/d; oral administration.
    ReferencesCancer Res. 2013 Feb 15;73(4):1386-99; Prostate. 2006 Dec 1;66(16):1768-78; Cancer Chemother Pharmacol. 2014 Jan;73(1):1-8. 


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

     

    Tasquinimod

    A. Chemical structure of tasquinimod (TasQ)  B. Comparison of anti-cancer efficacy of tasquinimod against CWR22-RH human prostate cancer xenografts. Cancer Res. 2013 Feb 15;73(4):1386-99. 
     

    Tasquinimod

    A. Tas-Q (1µM) and TSA (200nM) prevent lysine deacetylation in H3-histone at position 9 &19 induced by hypoxia in all of the human prostate cancer lines tested. β-actin was used as a loading control. B. Western blots of indicated HDAC in normal human prostate epithelial (i.e., 957E/hTERT) cells and LNCaP, PC-3, and DU-145 human PCs. Cancer Res. 2013 Feb 15;73(4):1386-99. 
     

    Tasquinimod

    A. HDAC4 increases and 1µM TasQ decreases HIF-1α protein in HEK-293T cells. β-actin was used as a loading control. B. TasQ lowers level of HDAC4 in the nuclei of LNCaPs in both normoxia and hypoxia. Cancer Res. 2013 Feb 15;73(4):1386-99. 


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