Cabotegravir (GSK1265744)

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

For research use only.

Catalog No.S7766 Synonyms: GSK744

5 publications

Cabotegravir (GSK1265744) Chemical Structure

CAS No. 1051375-10-0

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.

Selleck's Cabotegravir (GSK1265744) has been cited by 5 publications

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Biological Activity

Description

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

Kinase Assay: ^[1]	- Collapse 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: ^[1]	- Collapse 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. (Only for Reference)
Animal Research: ^[2]	- Collapse Animal Models: Rhesus macaques Dosages: 50 mg/kg Administration: -- (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	38 mg/mL warmed (93.74 mM)
	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 Download Cabotegravir (GSK1265744) SDF

Molecular Weight	405.35
Formula	C₁₉H₁₇F₂N₃O₅
CAS No.	1051375-10-0
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	GSK744
Smiles	CC1COC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O

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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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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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Integrase Signaling Pathway Map

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Cabotegravir (GSK1265744)