Home Microbiology Integrase inhibitor Cabotegravir (GSK1265744) For research use only.

Cabotegravir (GSK1265744)

Synonyms: GSK744, S/GSK1265744

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.

Cabotegravir (GSK1265744) Chemical Structure

Cabotegravir (GSK1265744) Chemical Structure

CAS No. 1051375-10-0

Purity & Quality Control

Cabotegravir (GSK1265744) Related Products

Signaling Pathway

Integrase Signaling Pathways

Integrase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T Antiviral assay 2 days Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days, IC50 = 0.0005 μM. 23845180
MT4 Antiviral assay 4 to 5 days Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells after 4 to 5 days by bioluminescence assay, IC50 = 0.0013 μM. 23845180
HEK293T Antiviral assay 2 days Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days in presence of human serum albumin, IC50 = 0.03 μM. 23845180
Click to View More Cell Line Experimental Data

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
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]
Kinase Assay 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 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.
In Vivo
In vivo GSK1265744 (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges. [2]
Animal Research Animal Models Rhesus macaques
Dosages 50 mg/kg
Administration --
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06319105 Recruiting
Oral Pre-exposure Prophylaxis (PrEP)|Long-acting Injectable Cabotegravir for PrEP
Georgetown University|AIDS Vaccine Advocacy Coalition|Centers for Disease Control and Prevention|Center for the Development of People|Cooper/Smith|Elizabeth Glaser Pediatric AIDS Foundation|Family Health Services|Healthqual|Johns Hopkins Research Project Malawi|Johns Hopkins Bloomberg School of Public Health|Kamuzu University of Health Sciences|Blantyre District Health Office Malawi|Lilongwe District Health Office Malawi|Lighthouse Trust|Ministry of Health Malawi|National AIDS Commission Malawi|Pakachere Institute of Health and Development Communication|Partners in Hope|Population Services International|University of North Carolina|United States Agency for International Development (USAID)|United States President''s Emergency Plan for AIDS Relief|Quantitative Engineering Design|Clinton Health Access Initiative-Malawi
 March 26 2024 --
NCT06104306 Recruiting
HIV-1-infection
Gilead Sciences
 December 13 2023 Phase 4
NCT05986084 Recruiting
Pre-Exposure Prophylaxis (PrEP)|Breast Feeding
Beth Israel Deaconess Medical Center|Botswana Harvard AIDS Institute Partnership|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|ViiV Healthcare
 November 30 2023 Phase 4

Chemical Information & Solubility

Molecular Weight 405.35 Formula

C19H17F2N3O5
CAS No. 1051375-10-0 SDF Download Cabotegravir (GSK1265744) SDF
Smiles CC1COC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 30 mg/mL ( (74.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

Handling Instructions

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