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Cabotegravir (GSK1265744)

Name: Cabotegravir (GSK1265744)
Brand: Selleck Chemicals
SKU: S7766
Rating: 5 (14 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: 1051375-10-0

Selleck's Cabotegravir (GSK1265744) has been cited by 14 publications

Purity & Quality Control

Batch: Purity: 99.90%

99.90

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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 2024-01-11)
NCT06104306	Recruiting	HIV-1-infection	Gilead Sciences	December 13 2023	Phase 4
NCT05986084	Not yet 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	October 2023	Phase 4
NCT05867212	Not yet recruiting	HIV Infections	Kelley-Ross & Associates Inc.	June 1 2023	--

References

Chemical lnformation & 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:

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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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