Home Metabolism IDO/TDO inhibitor Navoximod For research use only.

Navoximod

Synonyms: GDC-0919, NLG-919

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

Navoximod Chemical Structure

CAS No. 1402837-78-8

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Navoximod Related Products

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
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 toward B16-F10 cells in the presence of pretreatment with interferon (IFN)-γ in vitro.[3]
Cell Research 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% 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.
In Vivo
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]
Animal Research Animal Models C57BL/6 (H-2b, CD45.2) mice
Dosages 200 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02471846 Completed
Solid Tumor
Genentech Inc.
 July 28 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 316.37 Formula

C18H21FN2O2
CAS No. 1402837-78-8 SDF --
Smiles C1CC(CCC1C(CC2C3=C(C=CC=C3F)C4=CN=CN24)O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 63 mg/mL ( (199.13 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 63 mg/mL

Water : Insoluble


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In vivo
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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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