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[CAS NO. 1402837-78-8] Navoximod
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18770B |
| Brand: | MCE |
| CAS: | 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 |
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
DMSO : 100 mg/mL ( 316.09 mM ; Need ultrasonic)
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 |
-
1.
-
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.
-
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
References
- [1] Mario R. Mautino, et al. Abstract 491: NLG919, a novel indoleamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy. AACR 104th Annual Meeting 2013; Apr 6-10, 2013.
- [2] Li M, et al. The indoleamine 2,3-dioxygenase pathway controls complement-dependent enhancement of chemo-radiation therapy against murine glioblastoma. J Immunother Cancer. 2014 Jul 7;2:21.
- [3] Chen Y, et al. An immunostimulatory dual-functional nanocarrier that improves cancer immunochemotherapy. Nat Commun. 2016 Nov 7;7:13443.
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