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IDO-IN-2 IDO/TDO inhibitor

Name: IDO-IN-2
Brand: Selleck Chemicals
SKU: S7111
Availability: InStock
Rating: 5 (14 reviews)

Cat.No.S7111

IDO-IN-2 (RG 6078, NLG-919 analogue, GDC-0919 analogue) is a a potent IDO1 inhibitor with IC50 of 38 nM.

Chemical Structure

Molecular Weight: 282.38

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
HeLa	Function assay	Inhibition of IDO1 in IFNgamma-stimulated human HeLa cells incubated for 24 hrs, EC50=0.061 μM	26642377
HeLa	Function assay	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as inhibition of kynurenine production pre-incubated for 1 hr followed by IFN-gamma addition and measured after 18 hrs, IC50=0.004μM.	29398543
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	282.38	Formula	C₁₈H₂₂N₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1402836-58-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RG 6078, NLG-919 analogue, GDC-0919 analogue			Smiles	C1CCC(CC1)C(CC2C3=CC=CC=C3C4=CN=CN24)O

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (198.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 56 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.800mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 56 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.800mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 56 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	IDO1 ^[2] (Cell-free assay) 38 nM
In vitro	IDO-IN-2 (NLG-919 analogue, Compound 24) contains an imidazoleisoindole core and exhibits potent inhibitory activity to IDO1 with the IC50 value of 38 nM. This compound inhibits IDO activity with EC50 of 61 nM in HeLa cellular assay. The binding mode of this chemical to IDO1 is experimentally available and shows a direct coordinative interaction to the sixth coordination site of ferric heme.^[2] It has been used as reference compound in other studies to validate high-throughput screening assay for IDO1 inhibition and develop immunostimulatory nanomicellar carrier.^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/29031064/ [2] https://pubmed.ncbi.nlm.nih.gov/26642377/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02471846	Completed	Solid Tumor	Genentech Inc.	July 28 2015	Phase 1

Tech Support

Handling Instructions

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Frequently Asked Questions

Question 1:
This compound has two chiral centers, so which isoform (RR, RS, SR, SS) of it do you sell? Or it

Answer:
It is synthesized as a racemate, a mixture of four isoforms (RR, RS, SR, SS).

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