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    Lomeguatrib (PaTrin2)
    Lomeguatrib (PaTrin2)

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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 #: V0409
    CAS #: 192441-08-0Purity ≥98%

    Description: Lomeguatrib (formerly PaTrin-2) is a novel, potent and selective inhibitor of MGMT (O6-alkylguanine-DNA-alkyltransferase) with anticancer activity. It inhibits MGMT with IC50s of 9 nM and ∼6 nM in cell-free assay and MCF-7 cells, respectively.  

    References: J Med Chem. 1998;41(26):5265-71; Br J Cancer. 2005;93(10):1152-6; Int J Cancer. 2000;85(2):248-52.

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    Molecular Weight (MW)326.17
    FormulaC10H8BrN5OS
    CAS No.192441-08-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 65 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)NC1=NC(OCC2=CC(Br)=CS2)=C3N=CNC3=N1
    Synonyms

    PaTrin-2; Lomeguatrib; PaTrin 2; PaTrin2; 2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine

    InChi Key: JUJPKFNFCWJBCX-UHFFFAOYSA-N

    InChi Code: InChI=1S/C10H8BrN5OS/c11-5-1-6(18-3-5)2-17-9-7-8(14-4-13-7)15-10(12)16-9/h1,3-4H,2H2,(H3,12,13,14,15,16)

    SMILES Code: BrC1=CSC(COC2=C3N=CNC3=NC(N)=N2)=C1 


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    In Vitro

    In vitro activity: Lomeguatrib inactivates O6-alkylguanine-DNA-alkyltransferase (ATase) with a IC50 10-fold lower than O6-Benzylguanine. Lomeguatrib inhibits the activity of ATase in Raji cells with IC50 of 10 nM. Lomeguatrib effectively inactivates MGMT in MCF-7 cells with IC50 of ~6nM ). Lomeguatrib (10 μM ) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60= 10 μM with Lomeguatrib vs 400 μM without).


    Kinase Assay: Briefly, 200 μg of extracted cellular protein from HeLaS3 cells in 200 μL of 70 mM HEPES buffer (with 1 mM dithiothreitol (DTT), 5 mM EDTA, pH 7.8) is incubated at 37°C with a defined concentration of Lomeguatrib (added as a DMSO solution). After 30 min an excess of [3H]-methylated DNA(120 000 cpm) is added, and the incubation is continued for an additional 90 min. The reaction is stopped by the addition of 400 μL TCA (13%), and the DNA is hydrolyzed by heating the reaction mixture for 30 min at 98°C. The precipitated protein is washed three times with 400-μL portions of 5% TCA, solubilized in 0.1 N NaOH, and analyzed by liquid scintillation counting using the cocktail Rotiszint eco plus and a TRI-CARB. Enzyme activity is expressed as fmol of [3H]methyl transferred to TCA-insoluble protein material per mg of total cellular protein. Percent inhibition is calculated relative to untreated control samples. Each assay is repeated three times, and IC50 values are determined graphically from plots of percent inhibition vs inhibitor concentration


    Cell Assay: To determine toxicity, the MTT growth inhibition assay is employed. Cells (1000 per well) are plated into a 96-well plate and following a 24 hattachment period, Lomeguatrib is added to the cells. After 2 h incubation with Lomeguatrib (10 μM) at 37°C, 5% CO2, increasing doses of temozolomide or vehicle are added and the cells are incubated for a further 4-5 days. At the end of the exposure period, 150 μg MTT is added to each well and plates are incubated for 3 h at 37°C, 5% CO2. The media are removed and the formazan crystals formed in the viable cells are solubilised in 200 μL DMSO. The absorbances at 540 and 690 nm are determined using a ELISA plate reader and growth inhibition calculated as a percentage of the A540-A690 of untreated wells.

    In VivoLomeguatrib (20 mg/kg/day for 5 days) combined with temozolomide (100 mg/kg/day for 5 days) produces a substantial tumour growth delay: median tumour quintupling time is increased by 22 days without any significant increase in toxicity, while neither of the two drugs administrated along show any antitumor activity. Lomeguatrib inactivates ATase and enhances the anti-tumour effect of temozolomide in A375M human melanoma xenografts model. Lomeguatrib, at a single dose of 20 mg/kg i.p., produces complete ATase depletion in tumor within 2 hr. Temozolomide (100 g/kg/day) significantly delays growth of the A375M tumour xenograft with an estimated delay in the time for tumour to quintuple in size of 9.6 days. Addition of Lomeguatrib to temozolomide significantly enhances the latter’s effect, delaying the quintupling time a further 8.7 days. Moreover, the Lomeguatrib combination results in considerably less toxicity (0/9 vs. 2/9 deaths; 6.84% weight loss vs. 9.48%). Lomeguatrib alone has no significant effect on tumour growth.
    Animal modelNude mice with human breast tumour xenografts 
    Formulation & Dosage20 mg/kg; i.p.
    ReferencesJ Med Chem. 1998 Dec 17;41(26):5265-71; Br J Cancer. 2005 Nov 14;93(10):1152-6; Int J Cancer. 2000 Jan 15;85(2):248-52.


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

    Lomeguatrib

    Br J Cancer. 2005 Nov 14;93(10):1152-6.

    Lomeguatrib

    Br J Cancer. 2005 Nov 14;93(10):1152-6.

    Lomeguatrib

    Growth of MCF-7 tumour xenografts in nude mice. Br J Cancer. 2005 Nov 14;93(10):1152-6.


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