Cabotegravir (GSK744, GSK1265744)
Catalog No.S7766
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.
Cited by 2 publications
Purity & Quality Control
Choose Selective Integrase Inhibitors
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. | |
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| 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] |
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| In vivo | GSK1265744 (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges. [2] |
Protocol
| Kinase Assay: |
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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. |
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Solubility (25°C)
| In vitro | DMSO | 38 mg/mL warmed (93.74 mM) |
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| 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 |
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| Formula | C19H17F2N3O5 |
| CAS No. | 1051375-10-0 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT02799264 | Completed | Drug: Cabotegravir 30 mg | Infection Human Immunodeficiency Virus | ViiV Healthcare|Glaxosmithkline/Quintiles | June 2016 | Phase 1 |
| NCT02462772 | Withdrawn | Drug: cabotegravir|Drug: Placebo | Human Immunodeficiency Virus | Centre for the AIDS Programme of Research in South Africa|ViiV Healthcare | October 2015 | Phase 2 |
| NCT02354937 | Completed | Drug: GSK1265744 30 mg | Infection Human Immunodeficiency Virus|HIV Infections | ViiV Healthcare | July 13 2015 | Phase 1 |
| NCT02354950 | Completed | Drug: GSK1265744 30mg | HIV Infections | ViiV Healthcare|GlaxoSmithKline | June 22 2015 | Phase 1 |
Tech Support
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.
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