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NLG919
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NLG919图片
CAS NO:1402836-58-1
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
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1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)282.38
FormulaC18H22N2O
CAS No.1402836-58-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 15 mg/mL warmed (53.1 mM)
Water: <1 mg/mL
Ethanol: 30 mg/mL (106.2 mM)
SMILES CodeOC(C1CCCCC1)CC(C2=C3C=CC=C2)N4C3=CN=C4
SynonymsIDO-IN 7; IDO IN 7; RG6078 analog; GDC-0919; IDO IN-7; GDC0919 analog; GDC 0919; NLG919; NLG 919 analog; NLG-919; RG-6078; RG 6078.
实验参考方法
In Vitro

In vitro activity: NLG919 potently blocks IDO-induced T-cell suppression and restored robust T-cell responses with ED50 of 80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, NLG919 abrogated IDO-induced suppression of antigen-specific T cells (OT-I) in vitro, with ED50 of 120 NM.


Kinase Assay: IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM.


Cell Assay: 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.

In VivoIn mice, a single oral administration of NLG919 reduces the concentration of plasma and tissue Kyn by ~ 50%. In mice bearing B16F10 tumors, NLG919 markedly enhances the antitumor responses of naive, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA.
Animal modelMice bearing large established B16F10 tumor
Formulation & DosageDissolved in water at 3 mg/mL; 6 mg/day injected via IP, or administered subcutaneously at 1 mg/dose twice a day via injection plus 360 μg/day via an SC osmotic pump.
ReferencesJ Immunother Cancer. 2014 Jul 7;2:21; AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 491.