| Identification | Back Directory | [Name]
IDO-IN-7 | [CAS]
1402837-78-8 | [Synonyms]
IDO-IN-7
Navoximod
Navoximod (NLG919)
IDO-IN-7(Navoximod)
Reaxys ID: 22999399
Navoximod (GDC-0919
Navoximod (Synonyms: GDC-0919
GDC-0917;CUDC427;CUDC 427;GDC0917;GDC 0917
5H-Imidazo[5,1-a]isoindole-5-ethanol, 6-fluoro-α-(trans-4-hydroxycyclohexyl)-, (αR,5S)- | [Molecular Formula]
C18H21FN2O2 | [MDL Number]
MFCD29472253 | [MOL File]
1402837-78-8.mol | [Molecular Weight]
316.38 |
| Chemical Properties | Back Directory | [Boiling point ]
555.4±35.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);316.09(Max Conc. mM) | [form ]
Solid | [pka]
14.66±0.20(Predicted) | [color ]
White to light yellow | [InChI]
InChI=1/C18H21FN2O2/c19-14-3-1-2-13-16-9-20-10-21(16)15(18(13)14)8-17(23)11-4-6-12(22)7-5-11/h1-3,9-12,15,17,22-23H,4-8H2/t11-,12-,15-,17+/s3 | [InChIKey]
YGACXVRLDHEXKY-YYJRJVKZNA-N | [SMILES]
C([C@@H]1N2C=NC=C2C2=CC=CC(F)=C12)[C@H]([C@]1([H])CC[C@@H](O)CC1)O |&1:1,14,15,19,r| |
| Hazard Information | Back Directory | [Uses]
Navoximod (GDC-0919; NLG-?919) is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM. | [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 na?ve, 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]. | [IC 50]
IDO: 7 nM (Ki); IDO: 75 nM (EC50) | [storage]
Store at -20°C | [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. DOI:10.1186/2051-1426-2-21
[3] Chen Y, et al. An immunostimulatory dual-functional nanocarrier that improves cancer immunochemotherapy. Nat Commun. 2016 Nov 7;7:13443. DOI:10.1038/ncomms13443 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|