Cabotegravir (GSK744, GSK1265744)

Catalog No.S7766

Cabotegravir (GSK744, GSK1265744) Chemical Structure

Molecular Weight(MW): 405.35

Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.

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Biological Activity

Description Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.
Targets
HIV integrase [1]
In vitro

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. [1]

In vivo GSK1265744 (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges. [2]

Protocol

Kinase Assay:

[1]

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In vitro strand transfer 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 Research:

[1]

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  • Cell lines: Human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4)
  • Concentrations: ~20 μM
  • Incubation Time: --
  • Method:

    In vitro growth inhibition (cytotoxicity) studies are conducted with GSK1265744 in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as stimulated and unstimulated human PBMCs. As a surrogate of cell growth, ATP levels are quantified using CellTiter-Glo luciferase reagent.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Rhesus macaques
  • Formulation: --
  • Dosages: 50 mg/kg
  • Administration: --
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 38 mg/mL warmed (93.74 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 405.35
Formula

C19H17F2N3O5

CAS No. 1051375-10-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02720094 Recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID)|ViiV Healthcare|Gilead Sciences December 2016 Phase 2|Phase 3
NCT02478463 Not yet recruiting Infection, Human Immunodeficiency Virus ViiV Healthcare October 2016 Phase 1
NCT02938520 Recruiting Infection, Human Immunodeficiency Virus ViiV Healthcare|Janssen Pharmaceuticals|GlaxoSmithKline October 2016 Phase 3
NCT02951052 Recruiting Infection, Human Immunodeficiency Virus ViiV Healthcare|Janssen Pharmaceuticals|GlaxoSmithKline October 2016 Phase 3
NCT02799264 Completed Infection, Human Immunodeficiency Virus ViiV Healthcare|Glaxosmithkline/Quintiles June 2016 Phase 1
NCT02462772 Withdrawn Human Immunodeficiency Virus Centre for the AIDS Programme of Research in South Africa|ViiV Healthcare October 2015 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Integrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID