Linrodostat (BMS-986205)

Catalog No.S8629 Synonyms: ONO-7701

For research use only.

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

CAS No. 1923833-60-6

Selleck's Linrodostat (BMS-986205) has been cited by 4 Publications

Purity & Quality Control

Choose Selective IDO/TDO Inhibitors

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

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].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 410.91
Formula

C24H24ClFN2O

CAS No. 1923833-60-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1CCC(CC1)C2=C3C=C(C=CC3=NC=C2)F)C(=O)NC4=CC=C(C=C4)Cl

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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.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03936374 Completed Drug: BMS-986205|Drug: omeprazole Healthy Bristol-Myers Squibb May 8 2019 Phase 1
NCT03362411 Completed Drug: BMS-986205 Healthy Volunteers Bristol-Myers Squibb November 9 2017 Phase 1
NCT03312426 Completed Drug: BMS-986205 Healthy Volunteers Bristol-Myers Squibb October 9 2017 Phase 1
NCT02658890 Completed Drug: BMS-986205|Drug: Nivolumab|Drug: Ipilimumab Advanced Cancer|Melanoma|Non-Small Cell Lung Cancer Bristol-Myers Squibb February 22 2016 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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