NLG919 Chemical Properties

Melting point:

143 - 146°C

Boiling point:

524.6±33.0 °C(Predicted)

Density 

1.27±0.1 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

Soluble in DMSO (up to 15 mg/ml)

form 

solid

pka

14.85±0.20(Predicted)

color 

White

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

NLG919 Usage And Synthesis

Description

(±)-NLG-919 is an indoleamine 2,3-dioxygenase (IDO) pathway inhibitor (K_i = 7 nM; EC₅₀ = 75 nM). (±)-NLG-919 inhibits IDO-induced T cell suppression and restores T cell response during allogenic mixed lymphocyte reactions in vitro (ED₅₀s = 80 and 120 nM, respectively). In vivo, (±)-NLG-919 induces a 95% reduction in tumor volume when administered in conjunction with a pmel-1 T cell vaccine. Formulations containing (±)-NLG-919 are under investigation in clinical trials for treatment of glioblastoma, melanoma, pancreatic, and breast cancers.

Uses

NLG919 is a potent indoleamine-2,3-dioxygenase (IDO) pathway inhibitor and is suitable for the treatment of immunosuppression associated with cancer.

target

IDO pathway

References

1) Mautino?et al.?(2013),?NLG919, a novel indolamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy;?Cancer Res.?73?issue 8 supplement?491 2) Li?et al.?(2014),?The indolamine 2,3-dioxygenase pathway controls complement-dependent enhancement of chemo-radiation therapy against murine glioblastoma;?J. Immunother. Cancer?2?21 3) Meng?et al.?(2017),?Combinatorial antitumor effects of indoleamine 2,3-dioxygenase inhibitor NLG919 and paclitaxel in a murine B16-F10 melanoma model;?Int. J. Immunopathol. Pharmacol.?30?215

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