NLG919 (RG6078), IDO Inhibitor
Overview | |
Catalog # | bs-60258c-2-mg-solid |
Product Name | NLG919 (RG6078), IDO Inhibitor |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 282.38 Formula: C18 H22 N2 O CAS Number: 1402836-58-1 InChi Key: YTRRAUACYORZLX-UHFFFAOYSA-N InChi: InChI=1S/C18H22N2O/c21-18(13-6-2-1-3-7-13)10-16-14-8-4-5-9-15(14)17-11-19-12-20(16)17/h4-5,8-9,11-13,16,18,21H,1-3,6-7,10H2 Smiles: OC(CC1C2=CC=CC=C2C2=CN=CN21)C1CCCCC1 Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid Power. Shelf Life: 1.0 years |
Description | NLG919 is a potent, selective and orally bioavailable IDO (indoleamine-(2, 3)-dioxygenase) pathway inhibitor with Ki ~7 nM (EC50 ~75 nM) in vitro and in cell based assays. Oral administration of NLG919 reduces the [Kyn] in plasma and tissue by ~ 50%. Using human IDO+ pDCs in allogeneic MLR reactions, NLG919 potently blocked IDO- induced T cell suppression and restored robust T cell responses with an EC50 ~90 nM. NLG919 abrogated 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 mice bearing large established B16F10 tumors, administration of NLG919 markedly enhanced the antitumor responses of naïve, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA. Currently NLG919 is in phase I trial for the treatment of immunosuppression associated with cancer. |