NLG919
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.
NLG919是一种新型的、可口服的吲哚胺2,3-双加氧酶(IDO)途径的小分子抑制剂。Ki和EC50值分别为7 nM和75 nM。IDO途径是参与过敏性炎症的重要通路,通过将色氨酸(Trp)代谢合成犬尿氨酸(kynurenine)介导免疫抑制效应,分别经由GCN2、mTOR和AHR诱导下游信号,从而影响T细胞的增值和分化。由于IDO途径与各种恶性肿瘤的既定相关性,NLG919被用于与癌症相关的免疫抑制的治疗。
参考文献:
Mario R. Mautino, Firoz A. Jaipuri, Jesse Waldo, Sanjeev Kumar, James Adams, Clarissa Van Allen, Agnieszka Marcinowicz-Flick, David Munn, Nicholas Vahanian, Charles J. Link. NLG919, a novel indoleamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 491. doi:10.1158/1538-7445.AM2013-491
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 282.38 |
Cas No. | 1402836-58-1 |
Formula | C18H22N2O |
Solubility | insoluble in H2O; insoluble in EtOH; ≥47.7 mg/mL in DMSO |
Chemical Name | 1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol |
SDF | Download SDF |
Canonical SMILES | C1CCC(CC1)C(CC2C3=CC=CC=C3C4=CN=CN24)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 |
人和鼠IDO+ pDCs |
制备方法 |
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℃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℃可放置数月。 |
反应条件 |
37℃ |
实验结果 |
NLG919有效地阻断IDO诱导的T细胞抑制,恢复强有力的T细胞应答,EC50为90 nM。在来自小鼠肿瘤引流淋巴结的IDO+ pDCs中,NLG919消除了体外IDO诱导的抗原特异性T细胞(OT-I或pmel-1)的抑制,ED50为130 nM。 |
动物实验[1]: | |
动物模型 |
携带B16F10肿瘤小鼠 |
给药剂量 |
NLG919以3 mg/mL溶于水中给药,同时IP注射6 mg的日剂量或1 mg/dose,每天两次,皮下注射,同时SC渗透泵注射360 μg/day。 |
实验结果 |
在同源hgp100肽加上CpG-1826接种的幼稚pmel-1细胞IFA中,NLG919显著增强了抗肿瘤应答。NLG919加pmel-1/疫苗在接种的4天内,肿瘤大小显著减小。与接受pmel-1/疫苗没有使用NLG919的对照动物相比,肿瘤体积减少约95%。 |
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. Mario R. Mautino, Firoz A et al. NLG919, a novel indoleamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 491. |
描述 | NLG919是一个有效的吲哚胺-2,3-双加氧酶(indoleamine-2,3-dioxygenase,IDO)途径的抑制剂,Ki值为7 nM。 | |||||
靶点 | IDO pathway | |||||
IC50 | 7 nM (Ki) |
质量控制和MSDS
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