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Navoximod

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产品编号 TQ0071Cas号 1402837-78-8
别名 NLG-​919, GDC-0919

Navoximod (GDC-0919) 是 IDO(indoleamine-(2,3)-dioxygenase) 抑制剂,Ki=7 nM/,EC50=75 nM。

Navoximod

Navoximod

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纯度: 99.37%
产品编号 TQ0071 别名 NLG-​919, GDC-0919Cas号 1402837-78-8

Navoximod (GDC-0919) 是 IDO(indoleamine-(2,3)-dioxygenase) 抑制剂,Ki=7 nM/,EC50=75 nM。

规格价格库存数量
1 mg¥ 926现货
5 mg¥ 2,990现货
10 mg¥ 4,330现货
25 mg¥ 6,590现货
50 mg¥ 8,290现货
100 mg¥ 11,600现货
1 mL x 10 mM (in DMSO)¥ 3,230现货
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产品介绍

生物活性
产品描述
Navoximod (GDC-0919) (NLG- 919, GDC-0919) is a potent indoleamine-(2,3)-dioxygenase (IDO) pathway inhibitor (Ki/EC50: 7 nM/75 nM).
靶点活性
IDO:7 nM (Ki), IDO:75 nM (EC50)
体外活性
在异基因混合淋巴细胞反应(MLR)中,使用表达IDO的人源单核细胞来源的树突状细胞(DCs),Navoximod强力阻断IDO引起的T细胞抑制并恢复强烈的T细胞反应(ED50:80 nM)。同样,使用来自肿瘤引流淋巴结的表达IDO的小鼠DCs,Navoximod在体外消除IDO引起的特异性T细胞(OT-I)抑制(ED50:120 nM)[1]。Navoximod以浓度依赖的方式抑制IDO活性,其EC50为0.95μM。与游离的Navoximod相比,PEG2k-Fmoc-NLG(L)在抑制IDO方面活性较低(EC50:3.4μM),而PEG2k-Fmoc-NLG(S)活性最低(EC50>10μM)。将表达IDO的肿瘤细胞与来自BALB/c小鼠的脾细胞共培养会显著抑制T细胞的增殖。这种抑制在用Navoximod处理混合细胞时显著减弱。PEG2k-Fmoc-NLG(L)也能逆转肿瘤细胞的抑制效果,尽管其潜力略低于Navoximod[3]。
体内活性
在小鼠中,单次口服Navoximod可将血浆和组织中的Kyn浓度降低约50%。体内实验显示,在携带大型B16F10肿瘤的小鼠中,Navoximod的使用显著增强了未激活的pmel-1细胞对含hgp100多肽及CpG-1826的IFA疫苗的抗肿瘤反应。在这个严格的已建立肿瘤模型中,Navoximod加上pmel-1/疫苗的组合在接种后的4天内显著减少肿瘤体积(与仅接受pmel-1/疫苗而不使用Navoximod的对照动物相比,肿瘤体积减少约95%)[1]。当Navoximod与Temozolomide(TMZ)+放射治疗(RT)结合使用时,相对于仅用TMZ+RT治疗的小鼠,Navoximod和1-甲基-D-色氨酸(D-1MT,indoximod)均能提高生存率[2]。
细胞实验
Briefly, HeLa cells are seeded in a 96-well plate at a cell density of 5000 cells per well and allowed to grow overnight. Recombinant human IFN-γ is then added to each well with a final concentration of 50?ng/mL. At the same time, various concentrations of PEG2k-Fmoc-NLG(L), PEG2k-Fmoc-NLG(S) or Navoximod (NLG919) (50?nM-20?μM) are added to the cells. After 48?h of incubation, 150?μL of the supernatants per well is transferred to a new 96-well plate. Seventy-five μL of 30% trichloroacetic acid is added into each well and the mixture is incubated at 50°C for 30?min to hydrolyse N-formylkynurenine to kynurenine. For the colorimetric assay, supernatants are transferred to a new 96-well plate, mixed with an equal volume of Ehrlich reagent (2% p-dimethylamino-benzaldehyde w/v in glacial acetic acid), and incubated for 10?min at RT. The reaction product is measured at 490?nm by a plate reader [3].
动物实验
Mice are anesthetized with 4% isoflurane, and the surgical plane of anesthesia is maintained with 2% isoflurane in oxygen. Mice are immobilized in a stereotactic frame for tumor implantation. Briefly, the skull is shaved and exposed with a 0.5 cm skin incision. With the antiseptic technique, 10^5 GL261 cells (suspended in 3 μL RPMI-1640) are injected at the following coordinates with respect to the bregma on the right side (antero-posterior, -2 mm; medio-lateral, 2 mm; dorsoventral, 3 mm). This placement reproducibly yielded tumor growth in a paracortical area of the posterolateral right frontal lobe. Tumor-bearing mice are treated with combinations of oral DL-1MT (2 mg/mL D-1MT mixed with 2 mg/mL L-1MT) in drinking water, D-1MT (4 mg/mL) in drinking water, Navoximod (6 mg/mL) in drinking water, intraperitoneal cyclophosphamide, intraperitoneal temozolomide, and/or total-body radiation (500 cGy from a 137Cs source), as detailed in figure legends. Mice are observed daily and sacrificed when they became ill or moribund [2].
别名NLG-​919, GDC-0919
化学信息
分子量316.37
分子式C18H21FN2O2
CAS No.1402837-78-8
Smiles[H][C@@]1(CC[C@H](O)CC1)[C@H](O)C[C@H]1c2c(cccc2F)-c2cncn12
密度1.42 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 100 mg/mL (316.09 mM), Sonication is recommended.
溶液配制表
1mg5mg10mg50mg
1 mM3.1609 mL15.8043 mL31.6086 mL158.0428 mL
5 mM0.6322 mL3.1609 mL6.3217 mL31.6086 mL
10 mM0.3161 mL1.5804 mL3.1609 mL15.8043 mL
20 mM0.1580 mL0.7902 mL1.5804 mL7.9021 mL
50 mM0.0632 mL0.3161 mL0.6322 mL3.1609 mL
100 mM0.0316 mL0.1580 mL0.3161 mL1.5804 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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