Dolutegravir (GSK1349572)

Catalog No.S2667 Synonyms: S/GSK1349572

For research use only.

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.

Dolutegravir (GSK1349572) Chemical Structure

CAS No. 1051375-16-6

Selleck's Dolutegravir (GSK1349572) has been cited by 23 publications

Purity & Quality Control

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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 NFLrR5hHfW6ldHnvckBie3OjeR?= MoXPTY5pcWKrdHnvckBw\iCqdX3hckBQS1R{IHX4dJJme3OnZDDpckBOTEONMjDj[YxteyC3c3nu[{BcOTSFXX3leIZwem2rbjDhd{B{fWK|dILheIUh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegZY5idHm|aYO= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF|MkOzOEc,OjNzM{KzN|Q9N2F-
HOS M3HRemFvfGm4aYLhcEBie3OjeR?= NH\6N2w{KGi{cx?= NH\rU5dCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZvMTDoZZJjd3Krbnege4lt\CC2eYDlJIlvfGWpcnHz[UBqdm[nY4Tl[EBqdiCqdX3hckBJV1NiY3XscJMheHKndILlZZRm\CC5aYToJINwdXCxdX7kJIZweiB|IHjyd{BjgSC|aX7ncIUuem:3bnSgTGlXNTFiaX7m[YN1cX[rdImgZZN{[XluIFXDOVAhRSByLkCwNVYh|ryPLh?= NHfQUoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNVY3Pyd-MkS5NFE3Pjd:L3G+
HEK293T NVLUO|dJSW62aY\pdoFtKGG|c3H5 NGTqNHAzKGSjeYO= MYTBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDwd4V2\G9iSIXtZY4hcW2vdX7v[IVncWOrZX7jfUB3cXK3czDpcoZm[3SnZDDpckBJTUt{OUPUJINmdGy|IHHmeIVzKDJiZHH5d{whUUN3MDC9JFAvODBzNzFOwG0v NVHpeWl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFUyQDBpPkKzPFQ2OThyPD;hQi=>
MT4 NGnSTYJCdnSrdnnyZYwh[XO|YYm= NY\UenJtPCC2bzC1JIRigXN? MnzORY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTJVu[W5iaX3teY5w\GWoaXPp[Y5kgSC4aYL1d{AyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIF3UOEBk\WyuczDh[pRmeiB2IITvJFUh\GG7czDifUBjcW:udX3pcoV{[2WwY3WgZZN{[XluIFnDOVAhRSByLkCwNkDPxE1w NFnoTJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OVE5OCd-MkO4OFUyQDB:L3G+
HOS MoH0RY51cX[rcnHsJIF{e2G7 NVr5PFdSOyCqcoO= M4Ds[2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JJJidHSnZ4LheolzNXKnc3nzeIFvfCCKSW[tNUBp[XKkb4LpcochcW62ZXfyZZNmKE5zNUXIJI12fGGwdDDpcoZm[3SnZDDpckBpfW2jbjDIU3Mh[2WubIOgdJJmfHKnYYTl[EB4cXSqIHPvcZBwfW6mIH\vdkA{KGi{czDifUB{cW6pbHWtdo92dmRiSFnWMVEhcW6oZXP0bZZqfHliYYPzZZktKEWFNUCgQUAxNjByM{[g{txONg>? NYLXSJFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFE3PjdpPkK0PVAyPjZ5PD;hQi=>
HOS NIi5S|FCdnSrdnnyZYwh[XO|YYm= M2jMcVMhcHK| NESwOphCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBz[Wy2ZXfyZZZqei2{ZYPpd5RidnRiSFnWMVEhcGG{Yn;ybY5oKGmwdHXndoF{\SC\MUSzVkBufXSjboSgbY5n\WO2ZXSgbY4hcHWvYX6gTG9UKGOnbHzzJJBz\XS{ZXH0[YQhf2m2aDDjc41xd3WwZDDmc5IhOyCqcoOgZpkhe2mwZ3zlMZJwfW6mIFjJWk0yKGmwZnXjeIl3cXS7IHHzd4F6NCCHQ{WwJF0hOC5yMESzJO69VS5? M{C1PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCxOlY4Lz5{NEmwNVY3PzxxYU6=
HOS NHjkZ45CdnSrdnnyZYwh[XO|YYm= MV6zJIhzew>? MmjFRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgdoFtfGWpcnH2bZIuemW|aYP0ZY51KEiLVj2xJIhiemKxcnnu[{BqdnSnZ4Lhd4UhTzF2MGOvVVE1QEhiZH;1ZoxmKG23dHHueEBqdm[nY4Tl[EBqdiCqdX3hckBJV1NiY3XscJMheHKndILlZZRm\CC5aYToJINwdXCxdX7kJIZweiB|IHjyd{BjgSC|aX7ncIUuem:3bnSgTGlXNTFiaX7m[YN1cX[rdImgZZN{[XluIFXDOVAhRSByLkCwOVgh|ryPLh?= MlWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEG2OlcoRjJ2OUCxOlY4RC:jPh?=
HOS M3W5T2FvfGm4aYLhcEBie3OjeR?= MlzpN{BpenN? MX\BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDJUnNVUS2{ZYPpd5RidnRiSFnWMVEhcGG{Yn;ybY5oKGmwdHXndoF{\SCUMk[zT{BufXSjboSgbY5n\WO2ZXSgbY4hcHWvYX6gTG9UKGOnbHzzJJBz\XS{ZXH0[YQhf2m2aDDjc41xd3WwZDDmc5IhOyCqcoOgZpkhe2mwZ3zlMZJwfW6mIFjJWk0yKGmwZnXjeIl3cXS7IHHzd4F6NCCHQ{WwJF0hOC5yMUGg{txONg>? MnG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEG2OlcoRjJ2OUCxOlY4RC:jPh?=
HOS NXfBXW9kSW62aY\pdoFtKGG|c3H5 NWLiV3VZOyCqcoO= M16zXGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGlPW1SLLYLld4l{fGGwdDDITXYuOSCqYYLic5JqdmdiaX70[Ydz[XOnIFexNVhTKG23dHHueEBqdm[nY4Tl[EBqdiCqdX3hckBJV1NiY3XscJMheHKndILlZZRm\CC5aYToJINwdXCxdX7kJIZweiB|IHjyd{BjgSC|aX7ncIUuem:3bnSgTGlXNTFiaX7m[YN1cX[rdImgZZN{[XluIFXDOVAhRSByLkCxN{DPxE1w M13sRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCxOlY4Lz5{NEmwNVY3PzxxYU6=
P4R5 MAGI NYm1NXJySW62aY\pdoFtKGG|c3H5 MWGyOEBpenN? Mlm1RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCrbn\lZ5Rm\CCrbjDDSFQwS1iFUkSvR2NTPSCneIDy[ZN{cW6pIHj1cYFvKFB2UkWgUWFIUSClZXzsd{BxemWrbnP1ZoF1\WRid3n0bEBk\WyuczDmc5IhOjRiaILzJIZwdGyxd3XkJIJ6KH[rcnHsJIlv\mWldHnvckBu\WG|dYLl[EBi\nSncjC0PEBpenNiYomgZoV1[S2pYXzhZ5Rwe2mmYYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjB{IN88UU4> M2\uW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEOxPVc3Lz5|MECzNVk4PjxxYU6=
P4R5 MWnBcpRqfmm{YXygZZN{[Xl? M2\3flI1KGi{cx?= MkHxRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCrbn\lZ5Rm\CCrbjDDSFQwS1iFUkSvR2NTPSCneIDy[ZN{cW6pIHj1cYFvKFB2UkWgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC4aYLhcEBz\XCuaXPheIlwdiCycnXpcoN2[mG2ZXSge4l1cCClZXzsd{Bnd3JiMkSgbJJ{KG[xbHzve4VlKGK7II\pdoFtKGmwZnXjeIlwdiCvZXHzeZJm\CCjZoTldkA1QCCqcoOgZpkh[mW2YT3nZYxi[3Sxc3nkZZNmKHKncH;yeIVzKGenbnWgZZN{NCCHQ{WwJF0hOC5yMjFOwG0v MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV{NUK3PUc,Ojh3MkWyO|k9N2F-
HEK293T MoKwRY51cX[rcnHsJIF{e2G7 M{T1SVIh\GG7cx?= MoHyRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgdJNmfWSxIFj1cYFvKGmvbYXuc4Rm\mmlaXXuZ5khfmm{dYOgbY5n\WO2ZXSgbY4hUEWNMkmzWEBk\WyuczDh[pRmeiB{IHThfZMhcW5icILld4Vv[2Vib3[gbJVu[W5ic3XyeY0h[WykdX3pckwhUUN3MDC9JFAvODJ{IN88UU4> MlyzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NEWxPFAoRjJ|OES1NVgxRC:jPh?=
MDCK2 NI\0VHdHfW6ldHnvckBie3OjeR?= MmfaTY5pcWKrdHnvckBw\iCqdX3hckBQS1R{IHX4dJJme3OnZDDpckBOTEONMjDj[YxteyC3c3nu[{BcOTSFXX3leIZwem2rbjDhd{B{fWK|dILheIUh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegZY5idHm|aYOsJGlEPTBiPTCxMlkh|ryPLh?= NVz3VGVZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxN|I{OzRpPkKzNVMzOzN2PD;hQi=>
Vero E6 NF32eXRCdnSrdnnyZYwh[XO|YYm= M2G2UlIh\GG7cx?= NWTmPFhUSW62aY\pdoFtKGWoZnnjZYN6KGGpYXnud5QhW0GUUz3Dc3YuOiBqc4TyZYlvKEKjdmDheFEqKGmwIG\ldo8hTTZiY3XscJMh[XO|ZYPz[YQh[nliaX7obYJqfGmxbjDv[kB3cXKjbDDSUmEhemWybHnjZZRqd25ibXXhd5Vz\WRiYomgVnQuWEOUIHHmeIVzKDJiZHH5d{whTUN3MDC9JFIzNjB2IN88UU4> NYq5[WMyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ{OUKxNU8oRkOqRV3CUFww[T5?
Vero E6 NGix[IJCdnSrdnnyZYwh[XO|YYm= NFqxT5MzKGSjeYO= MmfyRY51cX[rcnHsJIVn\mmlYXP5JIFo[Wmwc4SgV2FTWy2Fb2[tNkApe3S{YXnuJGJiflCjdEGpJIlvKF[ncn:gSVYh[2WubIOgZZN{\XO|ZXSgZpkhcW6qaXLpeIlwdiCxZjD2bZJidCCUTlGgdoVxdGmlYYTpc44hdWWjc4Xy[YQh[nliUmStVGNTKGGodHXyJFIh\GG7czygSWM6OCB;IESyMlgyKM7:TT6= MoPCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVIzQTJzMT:nQmNpTU2ETEyvZV4>
Assay
Methods Test Index PMID
Dose-response infectivity curves NL4.3IN(WT) / NL4.3IN(S230R) virus 29617824

Protocol (from reference)

Kinase Assay:

[2]

  • 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]

  • 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].

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 419.38
Formula

C20H19F2N3O5

CAS No. 1051375-16-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05122767 Not yet recruiting Drug: Dolutegravir|Drug: 3HP Tuberculosis|HIV The Aurum Institute NPC|Johns Hopkins University October 30 2022 Phase 1|Phase 2
NCT05069688 Not yet recruiting Drug: rifampicin Pediatric HIV Infection|Tuberculosis Infection Brigham and Women''s Hospital|APIN Public Health Initiatives|University of Cape Town January 1 2022 Phase 1
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

(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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