Home Metabolism IDO/TDO inhibitor Linrodostat (BMS-986205) For research use only.

Linrodostat (BMS-986205)

Synonyms: ONO-7701

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.

Linrodostat (BMS-986205) Chemical Structure

Linrodostat (BMS-986205) Chemical Structure

CAS No. 1923833-60-6

Purity & Quality Control

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

Linrodostat (BMS-986205) Related Products

Biological Activity

Description 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.
Targets
IDO1 [1]
(Cell-free assay)
1.7 nM
In vitro
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].
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

Chemical Information & Solubility

Molecular Weight 410.91 Formula

C24H24ClFN2O
CAS No. 1923833-60-6 SDF --
Smiles CC(C1CCC(CC1)C2=C3C=C(C=CC3=NC=C2)F)C(=O)NC4=CC=C(C=C4)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 82 mg/mL ( (199.55 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble


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In vivo
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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.
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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.

Handling Instructions

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