NLG919

目录号: GC13912纯度: >99.50%同义词: 1-环己基-2-(5H-咪唑并[5,1-A]异吲哚-5-基)乙醇,NLG-919 analogue; GDC-0919 analogue
An IDO pathway inhibitor

NLG919
Cas No.: 1402836-58-1
规格价格库存数量操作
10mg¥450.00现货
1
25mg¥810.00现货
1
50mg¥1,350.00现货
1
100mg¥2,250.00现货
1
10mM (in 1mL DMSO)¥495.00现货
1

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

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

实验参考方法 Experimental Reference Method

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.

Reaction Conditions

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.

Applications

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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1402836-58-1
同义词
1-环己基-2-(5H-咪唑并[5,1-A]异吲哚-5-基)乙醇,NLG-919 analogue; GDC-0919 analogue
化学名
1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol
SMILES
C1CCC(CC1)C(CC2C3=CC=CC=C3C4=CN=CN24)O
分子式
C18H22N2O
分子量
282.38 g/mol
溶解性
≥ 47.7 mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol