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NLG919Potent IDO pathway inhibitor

NLG919

Catalog No. A4373
Size Price Stock Qty
10mM (in 1mL DMSO) $115.00 In stock
10mg $105.00 In stock
50mg $380.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

NLG919

Biological Activity

Description NLG919 is a potent inhibitor of indoleamine-2,3-dioxygenase (IDO)-pathway with Ki value of 7 nM.
Targets IDO pathway          
IC50 7 nM (Ki)          

Protocol

Cell experiment [1]:

Cell lines

Human and mouse IDO+ pDCs

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

37oC

Applications

NLG919 potently blockes IDO-induced T cell suppression and restores robust T cell responses with an EC50=90 nM. NLG919 also abrogates IDO-induced suppression of antigen-specific T cells (OT-I or pmel-1) in vitro, (ED50=130 nM ) using mouse IDO+ pDCs from tumor-draining lymph nodes.

Animal experiment [1]:

Animal models

Mice bearing large established B16F10 tumor

Dosage form

NLG919 was dosed either dissolved in the water at 3 mg/mL, plus a daily dose of 6 mg injected via IP, or administered subcutaneously at 1 mg/dose twice a day via injection plus 360 μg/day via an SC osmotic pump.

Application

NLG919 markedly enhances the antitumor responses of naive, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA. NLG919 plus pmel-1/vaccine produces a dramatic collapse of tumor size within 4 days of vaccination (~95% reduction in tumor volume compared to control animals receiving pmel-1/vaccine alone without NLG919).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Mario R. Mautino, Firoz A et al. NLG919, a novel indoleamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 491.

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Chemical Properties

Cas No. 1402836-58-1 SDF Download SDF
Chemical Name 1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol
Canonical SMILES C1CCC(CC1)C(CC2C3=CC=CC=C3C4=CN=CN24)O
Formula C18H22N2O M.Wt 282.38
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

NLG919 is a novel and orally-bioavailable small-molecule inhibitor of indoleamine 2,3-dioxygenase (IDO) pathway, a crucial pathway involved in allergic inflammation that mediates immunosuppressive effects through metabolization of tryptophan (Trp) to kynurenine and affects differentiation and proliferation of T cells through inducing downstream signaling via GCN2, mTOR and AHR, with values of inhibition constant Ki and half maximal effective concentration EC50 of 7 nM and 75 nM respectively. Due to the established correlation of IDO pathway with various malignancies, the IDO pathway inhibition as well as its desirable pharmacological and biological properties potentiates NLG919 to be used for the treatment of immunosuppression associated with cancer.

Reference

Mario R. Mautino, Firoz A. Jaipuri, Jesse Waldo, Sanjeev Kumar, James Adams, Clarissa Van Allen, Agnieszka Marcinowicz-Flick, David Munn, Nicholas Vahanian, Charles J. Link. NLG919, a novel indoleamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 491. doi:10.1158/1538-7445.AM2013-491