Indoximod (NLG-8189)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Indoximod是吲哚胺2,3-双加氧酶(IDO)途径抑制剂.IDO是一种色氨酸分解代谢酶,肿瘤细胞用其建立免疫抑制的状态.[1]
通过对Foxp3+/CD4+/CD25+表型的检验,IDO的免疫抑制活性可导致T调节细胞的数量增加.Indoximod也可减少T调节细胞的数量[2].在MMTV-Neu小鼠中,研究者着眼于indoximod与紫杉醇共用和非共用的活性[3].多西他赛与indoximod共用比多西他赛单独疗法更具毒性.单次1200 mg剂量的indoximod几乎达到完全的肠道饱和,更高剂量并不会显著提高峰值血浆水平.Indoximod单一制剂I期试验证明其具有很好的口服生物利用度和温和的毒性属性,而不产生显著的骨髓抑制,且在每日二次口服高达2000 mg的剂量下仍未达到最大耐受剂量[1].
在LLC小鼠模型中,以indoximod阻断IDO可提高对抗原和树突细胞(DC)疫苗的获得性免疫应答.
参考文献:
[1]. Soliman HH, Jackson E, Neuger T et al. A first in man phase I trial of the oral immunomodulator, indoximod, combined with docetaxel in patients with metastatic solid tumors. Oncotarget. 2014 Sep 30;5 (18):8136-46.
[2]. Munn DH. Blocking IDO activity to enhance anti-tumor immunity. Front Biosci (Elite Ed). 2012 Jan 1;4:734-45.
[3]. Muller AJ, DuHadaway JB, Donover PS et al.Inhibition of indoleamine 2,3-dioxygenase, an immunoregulatory target of the cancer suppression gene Bin1, potentiates cancer chemotherapy. Nat Med. 2005 Mar;11(3):312-9. Epub 2005 Feb 13.
Storage | Store at -20°C |
M.Wt | 218.25 |
Cas No. | 110117-83-4 |
Formula | C12H14N2O2 |
Solubility | insoluble in DMSO; insoluble in EtOH; ≥1.12 mg/mL in H2O with gentle warming and ultrasonic |
Chemical Name | (E)-3'-methyl-3''-styryl-3,2':5',2'':5'',3'''-quaterpyridine |
SDF | Download SDF |
Canonical SMILES | OC([C@H](N)CC1=CN(C)C2=CC=CC=C21)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
Treg细胞 |
制备方法 |
在DMSO中的溶解度有限。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
0.05 mM |
实验结果 |
Indoximod显著抑制Treg细胞分化,对IL-10+ Treg细胞分化的抑制作用更为显著,但对TGF-β1+ Treg细胞没有影响。Treg细胞与经过Indoximod预处理的ESCs共同培养后显示出较弱的抑制功能。上述结果表明,吲哚胺2,3-双加氧酶-1 (IDO1) 参与子宫内膜异位症中的Treg细胞的分化与抑制功能。 |
动物实验 [2]: | |
动物模型 |
携带4T1肿瘤的小鼠 |
给药剂量 |
400 mg/kg;口服给药;每天2次,每周5次 |
实验结果 |
在携带4T1肿瘤的小鼠中,DL-Indoximod与Cyclophosphamide联合使用增强抗肿瘤免疫力。此外,上述联合用药显著减少肿瘤大少。与L-Indoximod和Cyclophosphamide组合相比,D-Indoximod与Cyclophosphamide联合使用显著延长生存期。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Wei C, Mei J, Tang L, Liu Y, Li D, Li M, Zhu X. 1-Methyl-tryptophan attenuates regulatory T cells differentiation due to the inhibition of estrogen-IDO1-MRC2 axis in endometriosis. Cell Death Dis. 2016 Dec 1;7(12):e2489. [2]. Hou DY, Muller AJ, Sharma MD, DuHadaway J, Banerjee T, Johnson M, Mellor AL, Prendergast GC, Munn DH. Inhibition of indoleamine 2,3-dioxygenase in dendritic cells by stereoisomers of 1-methyl-tryptophan correlates with antitumor responses. Cancer Res. 2007 Jan 15;67(2):792-801. |
质量控制和MSDS
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