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    Cabotegravir (GSK744; GSK1265744)
    Cabotegravir (GSK744; GSK1265744)

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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 #: V1835
    CAS #: 1051375-10-0Purity ≥98%

    Description: Cabotegravir (also known as GSK744, GSK1265744) is a potent, orally bioavailable and long-acting inhibitor of HIV integrase used for the treatment and prevention of HIV infection. It has a broad spectrum of activity against different HIV subtypes. Cabotegravir inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. In resistance passage experiments, integrase enzyme assays, and cellular assays with site-directed molecular (SDM) HIV clones resistant to other classes of anti-HIV-1 agents and earlier integrase strand transfer inhibitors, Cabotegravir showed efficient inhibition of HIV replication through inhibiting HIV integrase. It is an investigational new drug under development for the treatment of HIV infection.

    References: Antimicrob Agents Chemother. 2015 Jan;59(1):397-406; Sci Transl Med. 2015 Jan 14;7(270):270ra4.

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    Molecular Weight (MW)405.35
    FormulaC19H17F2N3O5 
    CAS No.1051375-10-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 38 mg/mL (93.7 mM)
    Water:<1 mg/mL 
    Ethanol:<1 mg/mL
    SMILES CodeC[[email protected]]1CO[[email protected]]2N1C(C3=C(O)C(C(C(NCC4=C(F)C=C(F)C=C4)=O)=CN3C2)=O)=O
    Synonyms

    GSK744; GSK-744; GSK 744; S/GSK1265744; S/GSK 1265744; S/GSK-1265744; Cabotegravir.

    Chemical Name: (3S,11aR)-N-(2,4-difluorobenzyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide 

    Exact Mass: 405.1136 


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    In Vitro

    In vitro activity: GSK1265744 inhibits HIV replication with EC50 of 0.22 nM and 0.34-1.3 nM against HIV-1 Ba-L and NL432, respectively. GSK1265744 produces cytotoxicity with CC50 of 6.4, 5.0, 9.2, and 13 μM in proliferating IM-9, U-937, MT-4, and Molt-4 cell lines, respectively.


    Kinase Assay: The inhibitory concentrations of GSK1265744 is measured in a strand transfer assay using recombinant HIV IN. A complex of integrase and biotinylated donor DNA–streptavidin-coated SPA beads is formed by incubating 2 μM purified recombinant integrase with 0.66 μM biotinylated donor DNA–4 mg/mL streptavidin-coated SPA beads in 25 mM sodium MOPS pH 7.2, 23 mM NaCl, and 10 mM MgCl2 for 5 minutes at 37°C. These beads are spun down and preincubated with diluted INSTIs for 60 minutes at 37°C. Next, [3H]-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction is incubated at 37°C for 25 to 45 minutes, which allowed for a linear increase in strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.


    Cell Assay: Using resistance passage experiments, integrase enzyme assays, and cellular assays with site-directed molecular (SDM) HIV clones resistant to other classes of anti-HIV-1 agents and earlier integrase strand transfer inhibitors, results showed that GSK1265744 efficiently inhibited HIV replication through inhibiting HIV integrase

    In VivoGSK1265744 (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges. 
    Animal modelIn female pigtail macaques model that intravaginal inoculated simian/human immunodeficiency virus twice a week for up to 11 weeks, GSK744 injection prevented the macaques from being infected by virus while placebo controls were infected after a 4 median vaginal challenges with SHIV which reminded that GSK744 may be a potential preexposure prophylaxis drug for prevention via inhibiting HIV integrase  
    Formulation & Dosage
    References

    Antimicrob Agents Chemother. 2015 Jan;59(1):397-406; Sci Transl Med. 2015 Jan 14;7(270):270ra4.


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

    Cabotegravir (GSK744, GSK1265744)

    Effects of inhibitors on various forms of viral DNA were evaluated separately with HIV-1 NL432-infected MT-4 cells to determine the amounts of integrated viral DNA (a), 2-LTR circular viral DNA (b), or total viral DNA (c). Antimicrob Agents Chemother. 2015 Jan;59(1):397-406.
     
     

    Cabotegravir (GSK744, GSK1265744)

    Long-term culture of infected MT-2 cells with escalating concentrations of INSTIs. Antimicrob Agents Chemother. 2015 Jan;59(1):397-406.


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