Navoximod

Catalog No.S8957 Synonyms: GDC-0919, NLG-919

For research use only.

Navoximod (GDC-0919, NLG-919) is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) pathway with Ki of 7 nM and EC50 of 75 nM.

Navoximod Chemical Structure

CAS No. 1402837-78-8

Selleck's Navoximod has been cited by 4 Publications

Purity & Quality Control

Choose Selective IDO/TDO Inhibitors

Biological Activity

Description Navoximod (GDC-0919, NLG-919) is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) pathway with Ki of 7 nM and EC50 of 75 nM.
Targets
IDO [1]
(Cell-free assay)
IDO [1]
(Cell-free assay)
7 nM(Ki) 75 nM(EC50)
In vitro

NLG919 potently blocks IDO-induced T-cell suppression and restored robust T-cell responses with ED50 of 80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, NLG919 abrogated IDO-induced suppression of antigen-specific T cells (OT-I) in vitro, with ED50 of 120 nM. [1]

NLG919 increases the cytotoxic activity of paclitaxel toward B16-F10 cells in the presence of pretreatment with interferon (IFN)-γ in vitro.[3]

In vivo

In mice, a single oral administration of NLG919 reduces the concentration of plasma and tissue Kyn by ~ 50%. In mice bearing B16F10 tumors, NLG919 markedly enhances the antitumor responses of naive, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA.[1]

Immune competent mice are injected orthotopically with genetically engineered murine glioma cells and treated with GDC-0919 alone or combined with RT. GDC-0919 demonstrates potent inhibition of this node and effectively crosses the blood brain barrier. Although GDC-0919 as a single agent does not demonstrate anti-tumor activity, it has a strong potential for enhancing RT response in glioblastoma, which is further augmented with a hypofractionated regimen.[2]

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: the murine melanoma cell line B16-F10
  • Concentrations: 100 nM
  • Incubation Time: 12 h, 24 h, 48 h, 72 h
  • Method:

    B16-F10 cells are diluted to 1 × 105 cells/mL with DMEM supplemented with 10% FBS and seeded at 2 mL per well into 6-well plates. The culture medium is replaced with fresh growth medium with or without 25 ng/mL IFN-γ for 10–12 h after seeding. After incubation with IFN-γ for 24 h, the medium is replaced with fresh medium containing 100 nM NLG919, 3 nM PTX, or a combination of 100 nM NLG919 and 3 nM PTX, and medium containing 0.1% DMSO is used as the vehicle treatment. PTX at 3 nM is a concentration with low inhibition rate (IR) of cell growth about 20%. At 0, 12, 24, 48, and 72 h after addition of drugs, cells are washed to remove dead cells and particles. Adherent cells are trypsinized and counted using a CountStar IC1000 Automated Cell Counter (Ruiyu-Biotech). Viability of the counted cells is confirmed by 0.1% trypan blue exclusion. The effect of NLG919 and PTX on the growth of cells is analyzed by plotting cell growth curves using viable cell numbers against time.

Animal Research:

[2]

  • Animal Models: C57BL/6 (H-2b, CD45.2) mice
  • Dosages: 200 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 316.37
Formula

C18H21FN2O2

CAS No. 1402837-78-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(CCC1C(CC2C3=C(C=CC=C3F)C4=CN=CN24)O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02471846 Completed Drug: Atezolizumab|Drug: GDC-0919 Solid Tumor Genentech Inc. July 28 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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