Dolutegravir (GSK1349572)

For research use only.

Catalog No.S2667 Synonyms: S/GSK1349572

19 publications

Dolutegravir (GSK1349572) Chemical Structure

CAS No. 1051375-16-6

Dolutegravir (GSK1349572, S/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.

Selleck's Dolutegravir (GSK1349572) has been cited by 19 publications

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Biological Activity

Description Dolutegravir (GSK1349572, S/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 M4fOU2Z2dmO2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJG9EXDJiZYjwdoV{e2WmIHnuJG1FS0t{IHPlcIx{KHW|aX7nJHsyPEOfbXX0[o9zdWmwIHHzJJN2[nO2cnH0[UBjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDhcoFtgXOrcx?= NHTsT4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{GzNlM{PCd-MkOxN|I{OzR:L3G+
HOS NFPGUHhCdnSrdnnyZYwh[XO|YYm= Mn;5N{BpenN? MY\BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYuOSCqYYLic5Jqdmdid3ns[EB1gXCnIHnueIVoemG|ZTDpcoZm[3SnZDDpckBpfW2jbjDIU3Mh[2WubIOgdJJmfHKnYYTl[EB4cXSqIHPvcZBwfW6mIH\vdkA{KGi{czDifUB{cW6pbHWtdo92dmRiSFnWMVEhcW6oZXP0bZZqfHliYYPzZZktKEWFNUCgQUAxNjByMU[g{txONg>? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMU[2O{c,OjR7MEG2Olc9N2F-
HEK293T NXr5cnQ1SW62aY\pdoFtKGG|c3H5 MVyyJIRigXN? M1rEPWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JJB{\XWmbzDIeY1idiCrbX31co9l\W[rY3nlcoN6KH[rcoXzJIlv\mWldHXkJIlvKEiHS{K5N3Qh[2WubIOgZYZ1\XJiMjDkZZl{NCCLQ{WwJF0hOC5yMEG3JO69VS5? MnTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NEWxPFAoRjJ|OES1NVgxRC:jPh?=
MT4 NFOxOZJCdnSrdnnyZYwh[XO|YYm= NXy2eFJtPCC2bzC1JIRigXN? MWPBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIeY1idiCrbX31co9l\W[rY3nlcoN6KH[rcoXzJFEhO0JiaX7m[YN1\WRiaX6gbJVu[W5iTWS0JINmdGy|IHHmeIVzKDRidH:gOUBl[Xm|IHL5JIJqd2y3bXnu[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDBwMECyJO69VS5? NFXU[2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OVE5OCd-MkO4OFUyQDB:L3G+
HOS MnX3RY51cX[rcnHsJIF{e2G7 NF3BdHk{KGi{cx?= NEHRfYtCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBz[Wy2ZXfyZZZqei2{ZYPpd5RidnRiSFnWMVEhcGG{Yn;ybY5oKGmwdHXndoF{\SCQMUW1TEBufXSjboSgbY5n\WO2ZXSgbY4hcHWvYX6gTG9UKGOnbHzzJJBz\XS{ZXH0[YQhf2m2aDDjc41xd3WwZDDmc5IhOyCqcoOgZpkhe2mwZ3zlMZJwfW6mIFjJWk0yKGmwZnXjeIl3cXS7IHHzd4F6NCCHQ{WwJF0hOC5yMEO2JO69VS5? NFrZXGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNVY3Pyd-MkS5NFE3Pjd:L3G+
HOS MlPMRY51cX[rcnHsJIF{e2G7 NInpdZI{KGi{cx?= NFvOZYhCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBz[Wy2ZXfyZZZqei2{ZYPpd5RidnRiSFnWMVEhcGG{Yn;ybY5oKGmwdHXndoF{\SC\MUSzVkBufXSjboSgbY5n\WO2ZXSgbY4hcHWvYX6gTG9UKGOnbHzzJJBz\XS{ZXH0[YQhf2m2aDDjc41xd3WwZDDmc5IhOyCqcoOgZpkhe2mwZ3zlMZJwfW6mIFjJWk0yKGmwZnXjeIl3cXS7IHHzd4F6NCCHQ{WwJF0hOC5yMESzJO69VS5? NUDvXXlJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFE3PjdpPkK0PVAyPjZ5PD;hQi=>
HOS NHHq[W5CdnSrdnnyZYwh[XO|YYm= NHWzbpA{KGi{cx?= MoT2RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgdoFtfGWpcnH2bZIuemW|aYP0ZY51KEiLVj2xJIhiemKxcnnu[{BqdnSnZ4Lhd4UhTzF2MGOvVVE1QEhiZH;1ZoxmKG23dHHueEBqdm[nY4Tl[EBqdiCqdX3hckBJV1NiY3XscJMheHKndILlZZRm\CC5aYToJINwdXCxdX7kJIZweiB|IHjyd{BjgSC|aX7ncIUuem:3bnSgTGlXNTFiaX7m[YN1cX[rdImgZZN{[XluIFXDOVAhRSByLkCwOVgh|ryPLh?= Ml[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEG2OlcoRjJ2OUCxOlY4RC:jPh?=
HOS MmDqRY51cX[rcnHsJIF{e2G7 NVLLWnVFOyCqcoO= NEH1fGlCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBKVlOWST3y[ZNqe3SjboSgTGlXNTFiaHHyZo9zcW6pIHnueIVoemG|ZTDSNlY{UyCvdYThcpQhcW6oZXP0[YQhcW5iaIXtZY4hUE:VIHPlcIx{KHC{ZYTy[YF1\WRid3n0bEBkd22yb4Xu[EBnd3JiMzDodpMh[nlic3nu[4xmNXKxdX7kJGhKXi1zIHnu[oVkfGm4aYT5JIF{e2G7LDDFR|UxKD1iMD6wNVEh|ryPLh?= M2HGUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCxOlY4Lz5{NEmwNVY3PzxxYU6=
HOS MnrwRY51cX[rcnHsJIF{e2G7 NUnpZok1OyCqcoO= M4rSXGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGlPW1SLLYLld4l{fGGwdDDITXYuOSCqYYLic5JqdmdiaX70[Ydz[XOnIFexNVhTKG23dHHueEBqdm[nY4Tl[EBqdiCqdX3hckBJV1NiY3XscJMheHKndILlZZRm\CC5aYToJINwdXCxdX7kJIZweiB|IHjyd{BjgSC|aX7ncIUuem:3bnSgTGlXNTFiaX7m[YN1cX[rdImgZZN{[XluIFXDOVAhRSByLkCxN{DPxE1w NFPob5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNVY3Pyd-MkS5NFE3Pjd:L3G+
P4R5 MAGI MWHBcpRqfmm{YXygZZN{[Xl? MYKyOEBpenN? NY[5clNDSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDpcoZm[3SnZDDpckBETDRxQ2jDVlQwS0OUNTDlfJBz\XO|aX7nJIh2dWGwIGC0VlUhVUGJSTDj[YxteyCycnXpcoN2[mG2ZXSge4l1cCClZXzsd{Bnd3JiMkSgbJJ{KG[xbHzve4VlKGK7II\pdoFtKGmwZnXjeIlwdiCvZXHzeZJm\CCjZoTldkA1QCCqcoOgZpkh[mW2YT3nZYxi[3Sxc3nkZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVAhRSByLkCyJO69VS5? NWTLU3Y1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|E6PzZpPkOwNFMyQTd4PD;hQi=>
P4R5 MoHoRY51cX[rcnHsJIF{e2G7 M{XYN|I1KGi{cx?= MkjYRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCrbn\lZ5Rm\CCrbjDDSFQwS1iFUkSvR2NTPSCneIDy[ZN{cW6pIHj1cYFvKFB2UkWgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC4aYLhcEBz\XCuaXPheIlwdiCycnXpcoN2[mG2ZXSge4l1cCClZXzsd{Bnd3JiMkSgbJJ{KG[xbHzve4VlKGK7II\pdoFtKGmwZnXjeIlwdiCvZXHzeZJm\CCjZoTldkA1QCCqcoOgZpkh[mW2YT3nZYxi[3Sxc3nkZZNmKHKncH;yeIVzKGenbnWgZZN{NCCHQ{WwJF0hOC5yMjFOwG0v M1jiW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUK1Nlc6Lz5{OEWyOVI4QTxxYU6=
HEK293T M1fXV2FvfGm4aYLhcEBie3OjeR?= NUnpc4h[OiCmYYnz M1f3VWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JJB{\XWmbzDIeY1idiCrbX31co9l\W[rY3nlcoN6KH[rcoXzJIlv\mWldHXkJIlvKEiHS{K5N3Qh[2WubIOgZYZ1\XJiMjDkZZl{KGmwIIDy[ZNmdmOnIH;mJIh2dWGwIIPldpVuKGGuYoXtbY4tKEmFNUCgQUAxNjB{MjFOwG0v NH3nSZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OVE5OCd-MkO4OFUyQDB:L3G+
MDCK2 Mk\uSpVv[3Srb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJG9EXDJiZYjwdoV{e2WmIHnuJG1FS0t{IHPlcIx{KHW|aX7nJHsyPEOfbXX0[o9zdWmwIHHzJJN2[nO2cnH0[UBjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OCB;IEGuPUDPxE1w MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF|MkOzOEc,OjNzM{KzN|Q9N2F-
Vero E6 MlrzRY51cX[rcnHsJIF{e2G7 MkLUNkBl[Xm| MYLBcpRqfmm{YXyg[YZncWOjY4mgZYdicW6|dDDTRXJUNUOxVj2yJEh{fHKjaX6gRoF3WGG2MTmgbY4hXmW{bzDFOkBk\WyuczDhd5Nme3OnZDDifUBqdmirYnn0bY9vKG:oII\pdoFtKFKQQTDy[ZBtcWOjdHnvckBu\WG|dYLl[EBjgSCUVD3QR3Ih[W[2ZYKgNkBl[Xm|LDDFR|UxKD1iMkKuNFQh|ryPLh?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlI6OjFzLze+R4hGVUKOPD;hQi=>
Vero E6 MofaRY51cX[rcnHsJIF{e2G7 M1HKdFIh\GG7cx?= MU\BcpRqfmm{YXyg[YZncWOjY4mgZYdicW6|dDDTRXJUNUOxVj2yJEh{fHKjaX6gRoF3WGG2MTmgbY4hXmW{bzDFOkBk\WyuczDhd5Nme3OnZDDifUBqdmirYnn0bY9vKG:oII\pdoFtKFKQQTDy[ZBtcWOjdHnvckBu\WG|dYLl[EBjgSCUVD3QR3Ih[W[2ZYKgNkBl[Xm|LDDFR|kxKD1iNEKuPFEh|ryPLh?= NIm0cnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjJ7MkGxM{c,S2iHTVLMQE9iRg>?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Dose-response infectivity curves
NL4.3IN(WT) / NL4.3IN(S230R) virus; 

PubMed: 29617824     


Dose-response infectivity curves in the presence of dolutegravir (DTG) for wild-type (WT) and S230R viruses. Data reflect viral resistance to DTG in TZM-bl cells. TZM-bl cells were infected with NL4.3IN(WT) or NL4.3IN(S230R) virus over 48 hours, and luciferase levels were measured. Infectivity of NL4.3IN(WT) virus is shown for comparison. Dose-response curves were produced from the compilation of 3 independent experiments, each performed in triplicate. Error bars indicate means (±standard errors of the mean). RLU, relative luminescence units.

29617824

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 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

Molecular Weight 419.38
Formula

C20H19F2N3O5

CAS No. 1051375-16-6
Storage powder
in solvent
Synonyms S/GSK1349572
Smiles CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04771754 Not yet recruiting Drug: Dolutegravir HIV-1-infection Chelsea and Westminster NHS Foundation Trust October 1 2021 Phase 1
NCT04166474 Not yet recruiting Drug: Dolutegravir Hiv|Tuberculosis Helen Reynolds|Infectious Disease Institute Kampala Uganda|Desmond Tutu HIV Centre|University of Liverpool October 2021 Phase 4
NCT05006170 Not yet recruiting Drug: DTG DT 20 mg|Drug: DTG DT 25 mg Pediatric HIV Infection Chulalongkorn University August 3 2021 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID