Biological Activity: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. How to Use: In vitro: NLG919 was used at 10 µM final concentration in various in vitro assays.In vivo: NLG919 was dosed to mice orally or through IP injection with different dose and schedule. Reference:
本公司网站所展示销售的产品仅供科研！
沪公网安备 31011202007337号
