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(NLG-8189;&1-Methyl-D-tryptophan)
Indoximod的分子结构式
Indoximod是一种IDO抑制剂, 并逆转IDO介导的免疫抑制。
Indoximod的价格及库存
10&mM&*&1&mL
MCE提供各种包装，敬请垂询。
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Indoleamine 2,3-Dioxygenase (IDO)
研究的其它产品
8-Nitrotryptanthrin is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 &M.
Ki & Target: 0.97&0.1 &M (hIDO2)[1]
IC50 & Target: 1.8&0.6 &M (hIDO2), 0.45&0.2 &M (U87-hIDO2)[1]
InVitro: The typtanthrin derivative 8-Nitrotryptanthrin (5i) is found to be a potent hIDO2 inhibitor with superior efficiency far better than that of the most frequently-used inhibitor L-1-MT. The IC50 values show that all nine tryptanthrin compounds display hIDO2 inhibitory activities, especially, the compound 8-Nitrotryptanthrin demonstrates much stronger inhibition (1.87 &M) than both L-1-MT (82.53 &M) and D-1-MT (262.75 &M). 8-Nitrotryptanthrin exhibits significant antitrypanosomal activity with EC50 of 0.82 &M[2]. 8-Nitrotryptanthrin has a microplate Alamar Blue assay (MABA) minimum inhibitory concentration (MIC) value of 0.032 &g/mL. 8-Nitrotryptanthrin also has a LORA MIC value of 2.4 &g/mL, while the majority of analogues lack LORA activity[3].
IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM, shows activity in Hela cell (IC50=12 nM).
IDO-IN-3 is a potent IDO inhibitor.
IDO-IN-4 is a potent IDO1 inhibitor with IC50 of 8 nM in human IDO1/HEK293 cells.
IC50 value: 8 nM
Target: IDO1
Detailed information refer to WOA1.
IDO-IN-5 is a potent human IDO inhibitor with IC50 of 1-10 &M.
IC50 value: 1-10 &M
Target: IDO
Detailed information refer to WOA1.
IDO-IN-6 is a potent human IDO inhibitor with IC50 of ＜1 &M.
IC50 value: 1-10 &M
Target: IDO
Detailed information refer to WOA1.
IDO-IN-7 is a potent human IDO inhibitor with IC50 of ＜1 &M.
IC50 value: 1-10 &M
Target: IDO
Detailed information refer to WOA1.
IDO-IN-8 is a potent human IDO inhibitor with IC50 of 1-10 &M.
IC50 value: 1-10 &M
Target: IDO
Detailed information refer to WOA1.
IDO5L is a potent IDO1 inhibitor with IC50 of 67 nM, has an IC50 of 19 nM in Hela cell.
IC50 value: 67 nM [3]
Target: IDO
INCB 024360 is a potent and novel indoleamine-2,3 dioxygenase (IDO)inhibitor with an IC 50 value &100 nM.
IC50 Value: &100 nM [1]
Target: Indoleamine-2,3-dioxygenase
IDO is an immunomodulatory enzyme produced by some alternatively activated macrophages and other immunoregulatory cells (also used as an immune subversion strategy by many tumors). Interferon-gamma has an antiproliferative effect on many tumor cells and inhibits intracellular pathogens such as Toxoplasma and chlamydia, at least partly because of the induction of indoleamine 2,3-dioxygenase.
NLG919 is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM.
IC50 value: 7 nM/75 nM(Ki/EC50)
Target: indoleamine-(2,3)-dioxygenase inhibitor
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. 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.
&-Lapachone(ARQ-501; beta-lapachone) is a naturally occurring quinone obtained from the bark of the lapacho tree (Tabebuia avellanedae) with cancer chemop potent inhibitor of IDO1(IC50=0.44 uM).
IC50 value: 0.44 uM (IDO1)
Target: IDO1 anticancer agent
in vitro: &-Lapachone markedly induced cell death without caspase activation. &-Lapachone increased PI uptake and HMGB-1 release to extracellular space, which are markers of necrotic cell death. Necrostatin-1 (a RIP1 kinase inhibitor) markedly inhibited &-lapachone-induced cell death and HMGB-1 release. In addition, &-lapachone activated poly (ADP-ribosyl) polymerase-1(PARP-1) and promoted AIF release, and DPQ (a PARP-1 specific inhibitor) or AIF siRNA blocked &-lapachone-induced cell death [1]. In H9C2 cells, &-lap-mediated elevation of AMPK activity was retarded when the level of Sirt1 was reduced by transfection of siRNA against Sirt1 [2]. &-lapachone was identified as a submicromolar inhibitor of IDO1. &-lapachone represents a &10-fold gain in potency over the basic 1,2-naphthoquinone pharmacophore [4]. beta-lapachone inhibits the catalytic activity of topoisomerase I from calf thymus and human cells [5].
in vivo: Oral administration of &-lap to ACS Tg mice significantly attenuated heart failure and inhibited myocardial accumulation of triacylglycerol. &-lap administration significantly increased the expression of genes associated with mitochondrial biogenesis and fatty acid metabolism that were down-regulated in ACS Tg hearts [2].& Intraocular administration of &-lapachone resulted in significant reduction in hypoxia-induced retinal neovascularization without retinal toxicity or perturbation of developmental retinal angiogenesis in mice [3].
Indoximod的生物活性
Indoximod is an IDO pathway inhibitor, and reverses IDO-mediated immune suppression.
Target: IDO
in vitro: Indoximod significantly reverses the suppression of T cells created by IDO-expressing dendritic cells, using both human monocyte-derived dendritic cells and murine dendritic cells isolated directly from tumor-draining lymph nodes. Indoximod activates a Trp sufficiency signal that stimulates mTOR, and relieves IDO-induced Trp deprivation as well as an autophagic response.
in vivo: In mouse models of transplantable melanoma and transplantable and autochthonous breast cancer, Indoximod enhances antitumor immunity in the setting of combined chemo-immunotherapy regimens.
参考CoA中推荐的条件进行储存。
C12H14N2O2
溶剂/溶解度
10 mM in DMSO, H2O: ＜ 6.4 mg/mL您的位置： &&
；1,3-O-二咖啡酰奎宁酸
起批量（瓶装、盒装）
￥3/瓶装、盒装
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24 瓶装、盒装
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1 瓶装、盒装
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本草迷标准品 Rauvotetraphylline B[3-[[4-（3-Ethoxy-2-hydroxypropoxy）phenyl]amino]-3-oxopropyl]dimethylsulfonium 4-methylbenzenesulfonate； IPD 1151T； Suplatast tosilate Suplatast tosylate4，4’-[（2-methoxy-1，4-phenylene）di-（1E）-2，1-ethenediyl]bisphenol Methoxy-X04（E）-N-（4-（3-chloro-4-fluorophenylamino）-3-cyano-7-ethoxyquinolin-6-yl）-4-（dimethylamino）but-2-enamide Pelitinib （EKB-569）4，4’-[（2-methoxy-1，4-phenylene）di-（1E）-2，1-ethenediyl]bisphenol Methoxy-X043-（2-Imidazo[1，2-b]pyridazin-3-ylethynyl）-4-methyl-N-[4-[（4-methyl-1-piperazinyl）methyl]-3-（trifluoromethyl）phenyl]-benzamide； AP24534 Ponatinib1-Methyl-D-tryptophan； Indoximod IDO Pathway inhibitor4-[2-（4-Amino；1,3-O-二咖啡酰奎宁酸-1，2，5-oxadiazol-3-yl） GSK-690693（±）-1， （±）-Blebbistatin11-deoxojervine EZSolution Cyclopamine5-（3-Methoxy-4-（（4-methoxybenzyl）oxy）benzyl）pyrimidine-2，4-diamine EZSolution GW2580Cholesterol Assay DMSO （2。5 ml） Dimethyl Sulfoxide； Cholesterol Assay DMSO
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3秒自动关闭窗口Product Description
Biological Activity
Description
Indoximod (NLG-8189), a methylated tryptophan, acts as an IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor, and reverses IDO-mediated immune suppression. Phase 2.
Indoximod significantly reverses the suppression of T cells created by IDO-expressing dendritic cells, using both human monocyte-derived dendritic cells and murine dendritic cells isolated directly from tumor-draining lymph nodes.
Indoximod activates a Trp sufficiency signal that stimulates mTOR, and relieves IDO-induced Trp deprivation as well as an autophagic response.
In mouse models of transplantable melanoma and transplantable and autochthonous breast cancer, Indoximod (400 mg/kg p.o.) enhances antitumor immunity in the setting of combined chemo-immunotherapy regimens.
Protocol(Only for Reference)
Animal Study:
Animal Models
Mouse B16F10 and 4T1 tumor models
Formulation
0.5% Tween 80/0.5% Methylcellulose (v/v) in water
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by&
Animal B Km
Animal A Km
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) &&
mouse Km(3)
&= 11.2 mg/kg
References
Clinical Trial Information( data from http://clinicaltrials.gov, updated on )
NCT Number
Recruitment
Conditions
Sponsor/Collaborators
Start Date
Not yet recruiting
Acute Myeloid Leukemia
NewLink Genetics Corporation
Phase 1|Phase 2
Recruiting
Non-small Cell Lung Cancer|Progression of Non-small Cell Lung Cancer|Non-small Cell Lung Cancer Recurrent
NewLink Genetics Corporation
January 2016
Phase 1|Phase 2
Recruiting
Glioblastoma Multiforme|Glioma|Gliosarcoma|Malignant Brain Tumor|Ependymoma|Medulloblastoma
NewLink Genetics Corporation
October 2015
Recruiting
Metastatic Pancreatic Adenocarcinoma|Metastatic Pancreatic Cancer
NewLink Genetics Corporation
August 2014
Phase 1|Phase 2
Recruiting
Metastatic Melanoma|Stage III Melanoma|Stage IV Melanoma
NewLink Genetics Corporation
Phase 1|Phase 2
Molecular Weight (MW)
C12H14N2O2
3 years -20℃powder
2 years -80℃in solvent
1-Methyl-D-tryptophan
Solubility (25°C) *
&1 mg/ml means slightly soluble or insoluble.
Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name
(R)-2-amino-3-(1-methyl-1H-indol-3-yl)propanoic acid
Customers Who Bought This Item Also Bought
Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.
INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Phase 2.
NLG919 is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM in cell-free assays. Phase 1.
Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.
Features:More potent than PD0325901 or AZD6244.
Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.
Features:First orally available inhibitor of Aurora A.
Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Indoximod - Jefferies
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