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.
CAS Number: 1402836-58-1
Molecular Weight: 282.38
Chemical Name: 1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
NLG919 was used at 10 µM final concentration in various in vitro assays.
NLG919 was dosed to mice orally or through IP injection with different dose and schedule.
- Li M, et al. The indoleamine 2,3-dioxygenase pathway controls complement-dependent enhancement of chemo-radiation therapy against murine glioblastoma. (2014) J Immunother Cancer. 2:21.
- Mautino M, et al. NLG919, a novel indoleamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy. (2013) AACR poster 491.
Products are for research use only. Not for human use.
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