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Cabotegravir (GSK1265744)

Name: Cabotegravir (GSK1265744)
Brand: Selleck Chemicals
SKU: S7766
Rating: 5 (16 reviews)

Synonyms: GSK744, S/GSK1265744

Catalog No.S7766 Purity:99.90%

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

CAS No. 1051375-10-0

Purity & Quality Control

Batch: Purity: 99.90%

99.90

Cabotegravir (GSK1265744) Related Products

Related Targets	HIV-1 Integrase HIV-2 Integrase HIV Integrase	Click to Expand
Related Products	MK-2048 BMS-707035	Click to Expand
Related Compound Libraries	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	Click to Expand

Signaling Pathway

Integrase Signaling Pathway

Cell Data

Cell Lines	Assay Type	Incubation Time	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

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
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 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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