research use only

Linrodostat (BMS-986205) IDO/TDO inhibitor

Name: Linrodostat (BMS-986205)
Brand: Selleck Chemicals
SKU: S8629
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8629

Linrodostat (BMS-986205, ONO-7701) is an irreversible inhibitor of IDO1 with an IC50 of 1.7 nM. It inhibits kynurenine production with IC50 values of 1.7, 1.1 and > 2000 in human HeLa, HEK293 expressing human IDO-1 and tryptophan-2, 3-dioxygenase cell-based assays.

Chemical Structure

Molecular Weight: 410.91

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S862901 DMSO]82 mg/mL]false]Ethanol]82 mg/mL]false]Water]Insoluble]false Purity: 99.89%

99.89

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR Hydroxylase PCSK9 OXPHOS ROR
Related Products	Epacadostat (INCB024360) IDO-IN-2 Indoximod Navoximod PF-06840003 LM10 IDO inhibitor 1 Epacadostat (INCB024360) analogue 680C91 GNF-PF-3777 LY-3381916 Erianin Coptisine chloride IDO-IN-1

Chemical Information, Storage & Stability

Molecular Weight	410.91	Formula	C₂₄H₂₄ClFN₂O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1923833-60-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ONO-7701			Smiles	CC(C1CCC(CC1)C2=C3C=C(C=CC3=NC=C2)F)C(=O)NC4=CC=C(C=C4)Cl

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (199.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 82 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.	2.050mg/ml (4.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 41 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.	2.050mg/ml (4.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 41 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.

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 ^[1] (Cell-free assay) 1.7 nM
In vitro	BMS-986205 exhibits potent inhibition of kynurenine (kyn) production in IDO1-HEK293 cells (IC50 = 1.1 nM) but not in TDO-HEK293 cells^[1]. It is an irreversible suicide inhibitor^[2].
References	[1] http://cancerres.aacrjournals.org/content/77/13_Supplement/CT116 [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6021761/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03936374	Completed	Healthy	Bristol-Myers Squibb	May 8 2019	Phase 1
NCT03362411	Completed	Healthy Volunteers	Bristol-Myers Squibb	November 9 2017	Phase 1
NCT03312426	Completed	Healthy Volunteers	Bristol-Myers Squibb	October 9 2017	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):