Elvitegravir (JTK-303)

For research use only.

Catalog No.S2001 Synonyms: GS-9137

23 publications

Elvitegravir (JTK-303) Chemical Structure

Molecular Weight(MW): 447.88

Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.

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10mM (1mL in DMSO) USD 160 In stock
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Selleck's Elvitegravir (JTK-303) has been cited by 23 publications

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Biological Activity

Description Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.
Targets
HIV-1 IIIB [1]
(Cell-free assay)
HIV-2 ROD [1]
(Cell-free assay)
HIV-2 EHO [1]
(Cell-free assay)
0.7 nM 1.4 nM 2.8 nM
In vitro

Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir suppresses the replication of HIV-1, including various subtypes and multiple-drug-resistant clinical isolates, and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. Elvitegravir inhibits the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. Elvitegravir inhibits the HIV replication at a step that occurs after reverse transcription but before proteolytic cleavage, consistent with the integration step. Elvitegravir inhibits the synthesis of strand transfer products with an IC50 of 54 nM. Elvitegravir blocks integration via the inhibition of IN-mediated strand transfer. [1] Elvitegravir inhibits the integration of the HIV-based vector used as a positive control for the luciferase assay with an EC50 of 0.8 nM, as observed in the MAGI assay with HIV-1IIIB. Elvitegravir suppresses the replication of MLV infection with IC50 of 5.8 nM as well as that of the primate retrovirus SIV (IC50 = 0.5 nM), revealing that IN inhibitors have antiviral activity against a broad range of retroviruses. EVG is active against HIV-1 and HIV-2 and has a serum-free antiviral IC50 of 0.3-0.9 nM in peripheral blood mononuclear cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human C8166 cells MYLGeY5kfGmxbjDhd5NigQ>? NVLCN3NiSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDMRWkhO0JiaX7m[YN1\WRiaX6gbJVu[W5iQ{ixOlYh[2WubIOgZZN{\XO|ZXSgZZMheHKxdHXjeIlwdiCjZ3HpcpN1KH[rcoXzMYlv\HWlZXSgZ5l1d3CjdHjpZ{Bm\m[nY4SgZpkhVVSWIHHzd4F6NCCHQ{WwQVAvOjFibl2= MWiyNVc3OzF2OR?=
MT4 cells NUjoe2djTnWwY4Tpc44h[XO|YYm= NYfhRolKSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdiCPVESgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC4aYL1d{1qdmS3Y3XkJIN6fG:yYYTobYMh\W[oZXP0JIJ6KE2WVDDhd5NigSxiRVO1NF0xNjN5IH7N M3PMdVE5PjZ3NUiw
human MT4 cells NYfYXGlSS3m2b4TvfIlkcXS7IHHzd4F6 MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWFQh[2WubIOgZpkhVVSWIHHzd4F6NCCFQ{WwQVEvOTVizszN NYPt[IlXOTh4NkW1PFA>

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 89 mg/mL (198.71 mM)
Ethanol 35 mg/mL (78.14 mM)
Water 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 447.88
Formula

C23H23ClFNO5

CAS No. 697761-98-1
Storage powder
in solvent
Synonyms GS-9137
Smiles COC1=CC2=C(C=C1CC3=C(F)C(=CC=C3)Cl)C(=O)C(=CN2C(CO)C(C)C)C(O)=O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02985996 Completed Drug: Truvada|Drug: Genvoya HIV Infections Emory University|Centers for Disease Control and Prevention February 6 2017 Phase 1
NCT02251236 Completed Drug: Stribild|Drug: Genvoya HIV University of California San Diego|Gilead Sciences|University at Buffalo January 2016 Not Applicable
NCT02600819 Completed Drug: E/C/F/TAF|Drug: B/F/TAF HIV-1 Infection Gilead Sciences December 14 2015 Phase 3
NCT02295384 Completed Other: Retrospective Audit HIV Holdsworth House Medical Practice|Gilead Sciences November 2014 --
NCT02219217 Completed Drug: Dolutegravir Elvitegravir and Cobicistat HIV St Stephens Aids Trust|ViiV Healthcare October 2014 Phase 1
NCT02199613 Completed Drug: Treatment simplification HIV Infection University of British Columbia|Gilead Sciences October 2014 Phase 4

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.

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Integrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID