Cabotegravir (GSK1265744)

Catalog No.S7766 Synonyms: GSK744, S/GSK1265744

For research use only.

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

Selleck's Cabotegravir (GSK1265744) has been cited by 8 Publications

Purity & Quality Control

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T MXzBcpRqfmm{YXygZZN{[Xl? NFfrfoQzKGSjeYO= MY\BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDwd4V2\G9iSIXtZY4hcW2vdX7v[IVncWOrZX7jfUB3cXK3czDpcoZm[3SnZDDpckBJTUt{OUPUJINmdGy|IHHmeIVzKDJiZHH5d{whUUN3MDC9JFAvODByNTFOwG0v M1zFblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OES1NVgxLz5{M{i0OVE5ODxxYU6=
MT4 NIXk[HdCdnSrdnnyZYwh[XO|YYm= M3O5R|QhfG9iNTDkZZl{ MVHBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIeY1idiCrbX31co9l\W[rY3nlcoN6KH[rcoXzJFEhO0JiaX7m[YN1\WRiaX6gbJVu[W5iTWS0JINmdGy|IHHmeIVzKDRidH:gOUBl[Xm|IHL5JIJqd2y3bXnu[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDBwMECxN{DPxE1w M{jk[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OES1NVgxLz5{M{i0OVE5ODxxYU6=
HEK293T MVrBcpRqfmm{YXygZZN{[Xl? MYKyJIRigXN? NGPMN3pCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBxe2W3ZH:gTJVu[W5iaX3teY5w\GWoaXPp[Y5kgSC4aYL1d{Bqdm[nY4Tl[EBqdiCKRVuyPVNVKGOnbHzzJIFnfGW{IEKg[IF6eyCrbjDwdoV{\W6lZTDv[kBpfW2jbjDz[ZJ2dSCjbHL1cYlvNCCLQ{WwJF0hOC5yMzFOwG0v NVfpenQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFUyQDBpPkKzPFQ2OThyPD;hQi=>
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 Research:

[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 Research:

[2]

  • Animal Models: Rhesus macaques
  • Dosages: 50 mg/kg
  • Administration: --

Solubility (25°C)

In vitro

DMSO 38 mg/mL warmed
(93.74 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 405.35
Formula

C19H17F2N3O5

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

In vivo Formulation Calculator (Clear solution)

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

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Calculation results:

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03422172 Completed Drug: Oral CAB|Drug: CAB LA HIV Infections ViiV Healthcare|PPD April 10 2018 Phase 1
NCT02799264 Completed Drug: Cabotegravir 30 mg Infection Human Immunodeficiency Virus ViiV Healthcare|Glaxosmithkline/Quintiles June 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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