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    G007-LK
    G007-LK

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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 #: V0307
    CAS #: 1380672-07-0Purity ≥98%

    Description: G007-LK is a novel, potent and specific tankyrase (TNKS) 1/2 inhibitor with potential anticancer activity. It inhibits TNKS 1/2 with IC50s of 46 nM and 25 nM, respectively. G007-LK reduced auto-poly-(ADP ribosy)lation of TNKS1 and TNKS2. It shows potent antiproliferative activity against various cancer cells and high in vivo antitumor efficacy as well. In Wnt3a-induced HEK 293 cells, G007-LK inhibited ST-Luc with IC50 value of 0.05 μM. In SW480 colorectal cancer cell line transfected with GFP-TNKS1, G007-LK induces highly dynamic and mobile degradasomes containing phosphorylated beta-catenin, beta-TrCP and ubiquitin. In the APC-mutant cell lines, G007-LK reduces cytosolic and nuclear β-catenin protein levels.

    References: J Med Chem. 2013 Apr 11;56(7):3012-23; Cancer Res. 2013 May 15;73(10):3132-44.

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    Molecular Weight (MW)529.96
    FormulaC25H16ClN7O3S
    CAS No.1380672-07-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (188.7 mM)        
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: (E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile

    InChi Key: HIWVLHPKZNBSBE-OUKQBFOZSA-N

    InChi Code: InChI=1S/C25H16ClN7O3S/c1-37(34,35)18-10-11-20(28-15-18)24-31-29-22(33(24)21-5-3-2-4-19(21)26)12-13-23-30-32-25(36-23)17-8-6-16(14-27)7-9-17/h2-13,15H,1H3/b13-12+

    SMILES Code: N#CC1=CC=C(C2=NN=C(/C=C/C3=NN=C(C4=NC=C(S(=O)(C)=O)C=C4)N3C5=CC=CC=C5Cl)O2)C=C1

    SynonymsG00 7LK; G007-LK; G007LK


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    In Vitro

    In vitro activity: G007-LK reduces Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thereby promoting β-catenin destabilization. G007-LK completely blocks ligand-driven Wnt/β-catenin signaling in cell culture and display approximately 50% inhibition of APC mutation–driven signaling in most CRC cell lines. G007-LK (0.2 μM) reduces the number of COLO-320DM cells in mitosis from 24% to 12% and decreases HCT-15 cells in S-phase from 28% to 18%. G007-LK suppresses colony formation in CRC lines COLO-320DM and SW403. G007-LK suppresses organoids growth with IC50 of 80 nM.


    Kinase Assay: G007-LK inhibitory activity at various doses (duplicates) is tested twice against TNKS1, TNSK2 Chemiluminescent Assay Kits, and the luminescence is measured on a GloMax Luminometer.


    Cell Assay: For colony formation assays, cells are seeded at 500 cells/well in 2 mL of medium. Cell line in triplicate wells is treated with either 0.06% DMSO or compound in 0.06% DMSO and incubated for up to 17 days or until colonies became sufficiently large to quantify, changing medium and compound every third day. Colonies are stained by adding 200 μL of 12 mM 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide to each well for 1 h, and colony numbers are quantitated with a GelCount scanner at 1200 dpi resolution.

    In VivoG007-LK exhibits antitumor efficacy in xenograft and genetically engineered CRC models. In the COLO-320DM model, G007-LK reduces tankyrases 1 and tankyrases 2 protein levels, stabilizes AXIN1 and AXIN2, and decreases β-catenin level. Wnt/β-catenin signaling is clearly inhibited in a dose-dependent manner in the efficacy study tumors as indicated by reduced expression of β-catenin–activated genes NKD1, APCDD1, and TNFRSF19 (TROY), as well as increased expression of β-catenin–repressed gene CLIC3. G007-LK treatment increases expression of KRT20 and TM4SF4 in COLO-320DM tumors. G007-LK (20 mg/kg twice daily) achieves 61% tumor growth inhibition. G007-LK reduces Wnt/β-catenin signaling and cell proliferation in normal intestine.
    Animal modelHuman APC –mutant CRC xenograft COLO-320DM
    Formulation & DosageDissolved in 15% DMSO, 17.5% Cremophor EL, 8.75% ethanol, 8.75% Miglyol 810N, 50% PBS; 20 mg/kg;  i.p. injection
    References

    J Med Chem. 2013 Apr 11;56(7):3012-23; Cancer Res. 2013 May 15;73(10):3132-44.


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

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