bs-60258C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

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.