貨號	規格	價格	上海	北京	武漢	南京
S83133-5mg	99.6%	￥800.00 S83133-5mg ￥800.00 現貨	5 5	-	-	-
S83133-10mg	99.6%	￥1500.00 S83133-10mg ￥1500.00 現貨	4 4	-	-	-
S83133-25mg	99.6%	￥3500.00 S83133-25mg ￥3500.00 現貨	5 5	-	-	-
S83133-100mg	≥98%	￥9000.00 S83133-100mg ￥9000.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Navoximod (GDC-0919, NLG-919) 是一種有效的 IDO (indoleamine-(2,3)-dioxygenase) 途徑的抑制劑，其Ki值為7 nM，EC50值為75 nM

產品描述：

Navoximod (GDC-0919, NLG-919) 是一種有效的 IDO (indoleamine-(2,3)-dioxygenase) 途徑的抑制劑，其Ki值為7 nM，EC50值為75 nM

靶點：

IDO(Cell-free assay):7 nM(Ki); IDO(Cell-free assay):75 nM(EC50);Indoleamine2,3-Dioxygenase(IDO)

體外研究：

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. NLG919 increases the cytotoxic activity of paclitaxel toward B16-F10 cells in the presence of pretreatment with interferon (IFN)-γ in vitro

體內研究：

In mice, a single oral administration of NLG919 reduces the concentration of plasma and tissue Kyn by ~ 50%. In mice bearing B16F10 tumors, NLG919 markedly enhances the antitumor responses of naive, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA. Immune competent mice are injected orthotopically with genetically engineered murine glioma cells and treated with GDC-0919 alone or combined with RT. GDC-0919 demonstrates potent inhibition of this node and effectively crosses the blood brain barrier. Although GDC-0919 as a single agent does not demonstrate anti-tumor activity, it has a strong potential for enhancing RT response in glioblastoma, which is further augmented with a hypofractionated regimen.

細胞實驗：

Cell lines: the murine melanoma cell line B16-F10 Concentrations: 100?nM Incubation Time: 12?h, 24?h, 48?h, 72?h Method: B16-F10 cells are diluted to 1?×?105 cells/mL with DMEM supplemented with 10% FBS and seeded at 2?mL per well into 6-well plates. The culture medium is replaced with fresh growth medium with or without 25?ng/mL IFN-γ for 10–12?h after seeding. After incubation with IFN-γ for 24?h, the medium is replaced with fresh medium containing 100?nM NLG919, 3?nM PTX, or a combination of 100?nM NLG919 and 3?nM PTX, and medium containing 0.1% DMSO is used as the vehicle treatment. PTX at 3?nM is a concentration with low inhibition rate (IR) of cell growth about 20%. At 0, 12, 24, 48, and 72?h after addition of drugs, cells are washed to remove dead cells and particles. Adherent cells are trypsinized and counted using a CountStar IC1000 Automated Cell Counter (Ruiyu-Biotech). Viability of the counted cells is confirmed by 0.1% trypan blue exclusion. The effect of NLG919 and PTX on the growth of cells

動物實驗：

Animal Models: C57BL/6 (H-2b, CD45.2) mice Dosages: 200 mg/kg Administration: Oral gavage

參考文獻：

1. Mario R. Mautino, et al. Abstract 491: NLG919, a novel indoleamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy.. Cancer Res 2013;73(8 Suppl):Abstract nr 491. 2. Pravin Kesarwani, et al. Tryptophan Metabolism Contributes to Radiation-Induced Immune Checkpoint Reactivation in Glioblastoma. Clin Cancer Res. 2018 Aug 1;24(15):3632-3643. 3. Xiangjing Meng, et al. Combinatorial antitumor effects of indoleamine 2,3-dioxygenase inhibitor NLG919 and paclitaxel in a murine B16-F10 melanoma model. Int J Immunopathol Pharmacol. 2017 Sep;30(3):215-226.

溶解性：

Soluble in DMSO、Ethanol

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	3.161 ml	15.804 ml	31.609 ml
5 mM	0.632 ml	3.161 ml	6.322 ml
10 mM	0.316 ml	1.58 ml	3.161 ml
50 mM	0.063 ml	0.316 ml	0.632 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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