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Navoximod

    
99.60%

Navoximod

源叶(MedMol)
S83133 一键复制产品信息
1402837-78-8
C18H21FN2O2
316.3699
Navoximod;GDC-0919; NLG-​919
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S83133-5mg买3赠1
99.60%

¥800.00

5 - - - -
S83133-10mg促销
99.60%

¥1500.00 ¥1200.00

4 - - - -
S83133-25mg促销
99.60%

¥3500.00 ¥2800.00

4 - - - -
S83133-100mg促销
≥98%

¥9000.00 ¥7200.00

货期:2-3天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: Navoximod (GDC-0919, NLG-919) 是一种有效的 IDO (indoleamine-(2,3)-dioxygenase) 途径的抑制剂,其Ki值为7 nM,EC50值为75 nM
靶点: IDO(Cell-free assay):7 nM(Ki); IDO(Cell-free assay):75 nM(EC50);Indoleamine2,3-Dioxygenase(IDO)
体外研究: 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
体内研究: 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.
细胞实验: 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
动物实验: Animal Models: C57BL/6 (H-2b, CD45.2) mice Dosages: 200 mg/kg Administration: Oral gavage
参考文献: 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
保存条件: -20℃
配置溶液浓度参考:
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: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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