Cabotegravir (GSK1265744)

Catalog No.S7766 Batch:S776606

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Technical Data

Formula

C19H17F2N3O5
Molecular Weight 405.35 CAS No. 1051375-10-0
Solubility (25°C)* In vitro DMSO 20 mg/mL (49.34 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Cabotegravir (GSK744, GSK1265744, S/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 (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[2]
  • Animal Models

    Rhesus macaques

  • Dosages

    50 mg/kg

  • Administration

    --

Selleck's Cabotegravir (GSK1265744) has been cited by 15 publications

An effective two-stage NMBzA-induced rat esophageal tumor model revealing that the FAT-Hippo-YAP1 axis drives the progression of ESCC [ Cancer Lett, 2024, 588:216813] PubMed: 38499266
Ultra-long-acting in-situ forming implants with cabotegravir protect female macaques against rectal SHIV infection [ Nat Commun, 2023, 14(1):708] PubMed: 36759645
Dose-Ranging Plasma and Genital Tissue Pharmacokinetics and Biodegradation of Ultra-Long-Acting Cabotegravir In Situ Forming Implant [ Pharmaceutics, 2023, 15(5)1487] PubMed: 37242729
Dose-Ranging Plasma and Genital Tissue Pharmacokinetics and Biodegradation of Ultra-Long-Acting Cabotegravir In Situ Forming Implant [ Pharmaceutics, 2023, 15(5)1487] PubMed: 37242729
Virus-Mimicking Polymer Nanoparticles Targeting CD169+ Macrophages as Long-Acting Nanocarriers for Combination Antiretrovirals [ ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c17415] PubMed: 34995059
Impact of combinations of clinically observed HIV integrase mutations on phenotypic resistance to integrase strand transfer inhibitors (INSTIs): a molecular study [ J Antimicrob Chemother, 2022, dkab498] PubMed: 35061879
Female Genital Fibroblasts Diminish the In Vitro Efficacy of PrEP against HIV [ Viruses, 2022, 14(8)1723] PubMed: 36016345
Drug Interactions in Lenacapavir-Based Long-Acting Antiviral Combinations [ Viruses, 2022, 14(6)1202] PubMed: 35746673
mTORC1-Mediated Angiogenesis is Required for the Development of Rosacea [ Front Cell Dev Biol, 2021, 9:751785] PubMed: 34993194
High-level resistance to bictegravir and cabotegravir in subtype A- and D-infected HIV-1 patients failing raltegravir with multiple resistance mutations [ J Antimicrob Chemother, 2021, dkab276] PubMed: 34453542

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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