[CAS NO. 1402837-78-8] Navoximod

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PRODUCTS SPECIFICATIONS [1402837-78-8]

Catalog

HY-18770B

Brand

MCE

CAS

1402837-78-8

DESCRIPTION [1402837-78-8]

Overview

MDL	MFCD29472253
Molecular Weight	316.37
Molecular Formula	C18H21FN2O2
SMILES	O[C@H](CC1)CC[C@]1([H])[C@H](O)C[C@@H]2N3C(C4=C2C(F)=CC=C4)=CN=C3

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

Summary

Navoximod (GDC-0919; NLG-919) is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with K _i / EC ₅₀ of 7 nM/75 nM.

IC50 & Target

IDO

7 nM (Ki)

IDO

75 nM (EC ₅₀ )

In Vitro

Using IDO-expressing human monocyte-derived dendritic cells (DCs) in allogeneic mixed lymphocyte reaction (MLR) reactions, Navoximod (NLG919) potently blocks IDO-induced T cell suppression and restores robust T cell responses with an ED ₅₀ =80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, Navoximod abrogates IDO-induced suppression of antigen-specific T cells (OT-I) in vitro, with ED ₅₀ =120 nM ^[1] . Navoximod inhibits the IDO activity in a concentration-dependent manner with an EC ₅₀ of 0.95 μM. PEG2k-Fmoc-NLG(L) is less active (EC ₅₀ of 3.4 μM) in inhibiting IDO compared with free Navoximod while PEG2k-Fmoc-NLG(S) is least active (EC ₅₀ >10 μM). Coculture of IDO+tumor cells with splenocytes isolated from BALB/c mice leads to significant inhibition of T-cell proliferation. This inhibition is significantly attenuated when the mixed cells are treated with Navoximod. PEG2k-Fmoc-NLG(L) is also active in reversing the inhibitory effect of tumour cells although slightly less potent than Navoximod ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VNavoximod (NLG919) is orally bioavailable (F>70%); and has a favorable pharmacokinetic and toxicity profile. In mice, a single oral administration of Navoximod reduces the concentration of plasma and tissue Kyn by ~50%. In vivo, in mice bearing large established B16F10 tumors, administration of Navoximod markedly enhances the anti-tumor responses of naïve, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA. In this stringent established-tumor model, Navoximod plus pmel-1/vaccine produce a dramatic collapse of tumor size within 4 days of vaccination (~95% reduction in tumor volume compare to control animals receiving pmel-1/vaccine alone without Navoximod) ^[1] . When combined with NSC 362856 (TMZ)+radiation therapy (RT), both Navoximod and D-1MT (Indoximod) enhance survival relative to mice treated with TMZ+RT alone ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02048709	Genentech, Inc.	Solid Tumor	April 2014	Phase 1
NCT02471846	Genentech, Inc.	Solid Tumor	July 28, 2015	Phase 1
NCT05469490	Luke, Jason, MD\|Lumos Pharma\|University of Pittsburgh	Advanced Solid Tumors	October 2022	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 316.09 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1609 mL	15.8043 mL	31.6086 mL
5 mM	0.6322 mL	3.1609 mL	6.3217 mL
10 mM	0.3161 mL	1.5804 mL	3.1609 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 3 mg/mL (9.48 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 3 mg/mL (9.48 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 3 mg/mL (9.48 mM); Clear solution
4.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution
5.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution
6.

Add each solvent one by one: 1% DMSO >> 99% saline

Solubility: ≥ 0.5 mg/mL (1.58 mM); Clear solution

* All of the co-solvents are available by MCE.