Art. -Nr.: HY-15683

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IDO5L

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IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC₅₀ of 67 nM.

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Reinheit: 99.65%
CAS. Nr.: 914471-09-3
Formel: C₉H₇ClFN₅O₂
Molecular Weight:271.64

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

IDO5L Chemical Structure

CAS. Nr.: 914471-09-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC₅₀ of 67 nM.

IC₅₀ & Target^[1]

IDO

67 nM (IC₅₀)

IDO

19 nM (IC₅₀, in HeLa cell)

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	14.88 μM Compound: IDO5L	Antiproliferative activity against human A2780 cells assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human A2780 cells assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 38754563]
B16	IC₅₀	1 μM Compound: 5l	Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by adjusted cell-based spectrophotometry Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by adjusted cell-based spectrophotometry	[PMID: 19507862]
B16	IC₅₀	46 nM Compound: 5l	Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by spectrophotometry Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by spectrophotometry	[PMID: 19507862]
HeLa	EC₅₀	19 nM Compound: 78	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability Antiproliferative activity against human HeLa cells assessed as reduction in cell viability	[PMID: 33569941]
HeLa	IC₅₀	0.058 μM Compound: Incyte-5l	Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs	[PMID: 31525930]
HeLa	IC₅₀	19 nM Compound: 2	Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs	[PMID: 28523098]
HeLa	IC₅₀	19 nM Compound: 5l	Inhibition of indoleamine 2,3-dioxygenase in IFN-gamma-stimulated human HeLa cells assessed as kynurenine formation by spectrophotometry Inhibition of indoleamine 2,3-dioxygenase in IFN-gamma-stimulated human HeLa cells assessed as kynurenine formation by spectrophotometry	[PMID: 19507862]
HK-2	IC₅₀	30.81 μM Compound: IDO5L	Cytotoxicity against HK-2 cells Cytotoxicity against HK-2 cells	[PMID: 38754563]
MDA-MB-231	EC₅₀	59 nM Compound: 5l	Inhibition of IDO1 in IFNgamma-induced human MDA-MB-231 cells using tryptophan as substrate preincubated for 4 hrs followed by substrate addition for 5 hrs by spectrophotometric method Inhibition of IDO1 in IFNgamma-induced human MDA-MB-231 cells using tryptophan as substrate preincubated for 4 hrs followed by substrate addition for 5 hrs by spectrophotometric method	[PMID: 27994758]
P815	IC₅₀	0.1 μM Compound: 5l	Inhibition of mouse IDO1 in P815 clone 6 cells by HPLC analysis Inhibition of mouse IDO1 in P815 clone 6 cells by HPLC analysis	[PMID: 22616902]
P815	IC₅₀	60 μM Compound: 5l	Inhibition of mouse TDO in P815 clone 12 cells by HPLC analysis Inhibition of mouse TDO in P815 clone 12 cells by HPLC analysis	[PMID: 22616902]

In Vitro

IDO5L (Compound 5l) is a potent (HeLa IC₅₀=19 nM) inhibitor of IDO^[1]. IDO5L is one of the highest potent inhibitors of the IDO1 (IC₅₀=19 nM, in HeLa cell assay)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Testing of IDO5L in mice demonstrates pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy in mice bearing GM-CSF-secreting B16 melanoma tumors. Initial oral pharmacokinetic studies show that IDO5L is rapidly cleared (t_1/2<0.5 h) and that oral administration will not be a suitable dosing method for in vivo studies. The measured plasma exposure (2.5 μM) of IDO5L during this period exceeded our calculated mouse protein binding adjusted B16 cellular IC₅₀ (PB_adjIC₅₀=1.0 μM, murine cellular B16 IC₅₀=46 nM). Notably, kynurenine levels increase back to baseline after 4 h as IDO5L exposure levels decreased below the mouse PB_adjIC₅₀ from 1.0 to 0.1 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 914471-09-3
Appearance Solid
Molecular Weight 271.64
Formel C₉H₇ClFN₅O₂
Color Off-white to yellow
SMILES

ON/C(C1=NON=C1N)=N/C2=CC=C(F)C(Cl)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Chem Sci

A tumor acidity activatable and Ca2+-assisted immuno-nanoagent enhances breast cancer therapy and suppresses cancer recurrence. [Abstract]

2020 Jun 29;11(28):7429-7437. PMID: 34123024
Pharmaceuticals (Basel)

Evaluation of Novel Inhibitors of Tryptophan Dioxygenases for Enzyme and Species Selectivity Using Engineered Tumour Cell Lines Expressing Either Murine or Human IDO1 or TDO2. [Abstract]

2022 Aug 31;15(9):1090. PMID: 36145311
Chem Commun (Camb)

Photothermal therapy-induced immunogenic cell death based on natural melanin nanoparticles against breast cancer. [Abstract]

2020 Jan 30;56(9):1389-1392. PMID: 31912821

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 52 mg/mL (191.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.6813 mL

18.4067 mL

36.8134 mL

5 mM

0.7363 mL

3.6813 mL

7.3627 mL

10 mM

0.3681 mL

1.8407 mL

3.6813 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (9.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (9.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[1]

Mice^[1]
A single subcutaneous 100 mg/kg dose of IDO5L is administered to naive C57BL/6 mice bearing GM-CSF-secreting B16 tumors. Blood is harvested from individual mice over 8 h. Kynurenine and IDO5L concentrations are measured by LCMS. Reductions of kynurenine levels by 50-60% are observed between 2 and 4 h, with maximum inhibition seen at 2.5 h. Tumors are allowed to grow until day 7 when 14 days of subcutaneous dosing of IDO5L at 25, 50, and 75 mg/kg b.i.d. is initiated. Dose dependent inhibition of tumor growth is correlated with increasing exposures of IDO5L in plasma.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yue EW, et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J Med Chem. 2009 Dec 10;52(23):7364-7. [Content Brief]

[2]. Huang X, et al. Synthesis of [(18) F] 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): a novel potential PET probe for imaging of IDO1 expression. J Labelled Comp Radiopharm. 2015 Apr;58(4):156-62. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6813 mL	18.4067 mL	36.8134 mL	92.0336 mL
	5 mM	0.7363 mL	3.6813 mL	7.3627 mL	18.4067 mL
	10 mM	0.3681 mL	1.8407 mL	3.6813 mL	9.2034 mL
	15 mM	0.2454 mL	1.2271 mL	2.4542 mL	6.1356 mL
	20 mM	0.1841 mL	0.9203 mL	1.8407 mL	4.6017 mL
	25 mM	0.1473 mL	0.7363 mL	1.4725 mL	3.6813 mL
	30 mM	0.1227 mL	0.6136 mL	1.2271 mL	3.0678 mL
	40 mM	0.0920 mL	0.4602 mL	0.9203 mL	2.3008 mL
	50 mM	0.0736 mL	0.3681 mL	0.7363 mL	1.8407 mL
	60 mM	0.0614 mL	0.3068 mL	0.6136 mL	1.5339 mL
	80 mM	0.0460 mL	0.2301 mL	0.4602 mL	1.1504 mL
	100 mM	0.0368 mL	0.1841 mL	0.3681 mL	0.9203 mL

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IDO5L

Human Metabolite Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Publications Citing Use of MedChemExpress (MCE) IDO5L

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IDO5L

Human Metabolite Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Publications Citing Use of MedChemExpress (MCE) IDO5L

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IDO5L Related Classifications

HY-15683 Related Classifications