Dolutegravir (GSK1349572)

Catalog No.S2667 Synonyms: S/GSK1349572

Dolutegravir (GSK1349572) Chemical Structure

Molecular Weight(MW): 419.38

Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

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In DMSO USD 450 In stock
USD 270 In stock
USD 370 In stock
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2 Customer Reviews

  • Strand transfer was carried out with RSV IN(1-269) (4 uM) and GU320R(2 uM)in the presence of 50mM NDSB201. Increasing concentrations of STIs were added as indicated at the top; DTG(Dolutegravir) in lanes 3-5, MK-2048 in lanes 6-8, and RAL in lanes 9-11. No STI was present in lane 2, and lane 1 contains the molecular weight markers. Strand transfer products and ODN substrate are identified on the right. CHS, circular half-site; OC target and SC target, open circular and supercoiled target DNA, respectively.

    J Biol Chem 2014 289(28), 19648-58. Dolutegravir (GSK1349572) purchased from Selleck.

    Comparison of the activity of dolutegravir (DTG), raltegravir (RAL), and elvitegravir (EVG) against wild-type HIV-2ROD9. The number of independent determinations (n) for each strain is shown below the x-axis. No cytotoxic effects were observed in dolutegravir-treated MAGIC-5A cultures at concentrations as high as 10,000 nM.

    Retrovirology, 2015, 10.1186/s12977-015-0146-8. Dolutegravir (GSK1349572) purchased from Selleck.

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Biological Activity

Description Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
Features A next-generation and two-metal-binding HIV integrase strand transfer inhibitor.
Targets
HIV integrase [2]
(Cell-free assay)
2.7 nM
In vitro

S/GSK1349572 shows the potent inhibitory effect on nine clinical isolates from integrase inhibitor-naive HIV-2-infected patients with EC50 ranging from 0.2 nM -1.4 nM. [1] In vitro, S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM. Furthermore, S/GSK1349572 potently inhibits HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector with EC50 of 0,51 nM, 0.71 nM and 2.2 nM, respectively. [2] In vitro, S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor--resistant or nucleoside reverse transcription inhibitor--resistant viruses with EC50 ranging from 1.3 nM -2.1 nM. Similarly to that against wild-type virus, S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses with EC50 of 0.36 nM and 0.37 nM, respectively. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDCK2 cells M2\YRWZ2dmO2aX;uJIF{e2G7 NH7FeVJKdmirYnn0bY9vKG:oIHj1cYFvKE:FVEKg[ZhxemW|c3XkJIlvKE2GQ1uyJINmdGy|IIXzbY5oKFtzNFPdcYV1\m:{bXnuJIF{KHO3YoP0doF1\SCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[{BidmGueYPpdy=> NGHYN4kzOzF|MkOzOC=>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[2]

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In vitro strand transfer assay:

The inhibitory potencies of S/GSK1349572 and other INIs are measured in a strand transfer assay using recombinant HIV integrase. A complex of integrase and biotinylated preprocessed donor DNA-streptavidin-coated Acintillation proximity assay (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 morpholinepropanesulfonic acid (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 INIs for 60 minutes at 37 °C. Then a 3H-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction mixture is incubated at 37 °C for 25 to 45 minutes, which allows for a linear increase in the strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.
Cell Research:

[2]

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  • Cell lines: MT-4
  • Concentrations: 0 to 10 μM
  • Incubation Time: 4 days or 5 days
  • Method:

    MT-4 cells growing exponentially at a density of 500000 or 600000 /mL are infected with HIV-1 strain IIIB at a viral multiplicity of infection of 0.001 or a 50% tissue culture infective dose of 4 to 10. The cells are then aliquoted to 96-well plates in the presence of varying concentrations of S/GSK1349572. After incubation for 4 or 5 days, antiviral activity is determined by a cell viability assay that either measured bioluminescence with a CellTiter-Glo luminescent reagent or measured absorbance at 560 and 690 nm using the yellow tetrazolium MTT reagent [3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide].


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL warmed (197.91 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or 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

Molecular Weight 419.38
Formula

C20H19F2N3O5

CAS No. 1051375-16-6
Storage powder
in solvent
Synonyms S/GSK1349572

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02771249 Suspended Healthy Volunteers National Institutes of Health Clinical Center (CC) May 5, 2016 Phase 1
NCT03048422 Not yet recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) April 30, 2017 Phase 3
NCT03017872 Not yet recruiting HIV Infections Kirby Institute|UNITAID|National Health and Medical Research Council, Australia|ViiV Healthcare|Janssen Pharmaceutica April 2017 Phase 4
NCT03016533 Not yet recruiting Infection, Human Immunodeficiency Virus ViiV Healthcare|PPD March 2017 Phase 3
NCT02987530 Not yet recruiting HIV-1 Infection French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Institut National de la Santé Et de la Recherche Médicale, France January 2017 Phase 3
NCT02976259 Not yet recruiting HIV Infection Primary Institut de Médecine et dEpidémiologie Appliquée - Fondation Internationale Léon MBa December 2016 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID