Other
CN
EU
USA
Description: NLG919 analog (also known as RG6078 analog; GDC0919 analog; IDO-IN-7; NLG-919 analogue; GDC-0919 analogue) is a novel, potent and orally bioavailable inhibitor of IDO (indoleamine-(2,3)-dioxygenase) pathway with Ki/EC50 of 7 nM/75 nM in cell-free assays. It has potential immunomodulating and antineoplastic activities. NLG919 targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the essential amino acid tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, this agent increases tryptophan levels, restores the proliferation and activation of various immune cells, including NK cells, T-lymphocytes, and causes a reduction in tumor-associated regulatory T-cells.
References: J Immunother Cancer. 2014 Jul 7;2:21; AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 491.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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.
Purity ≥98%
COA
MSDS
NMR