BMS-986205

Catalog No.S8629

BMS-986205 Chemical Structure

Molecular Weight(MW): 410.91

BMS-986205 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.

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Biological Activity

Description BMS-986205 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

Solubility (25°C)

In vitro DMSO 82 mg/mL (199.55 mM)
Ethanol 82 mg/mL (199.55 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 410.91
Formula

C24H24ClFN2O

CAS No. 1923833-60-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03854032 Not yet recruiting Lip|Oral Cavity Squamous Cell Carcinoma|Pharynx|Larynx|Squamous Cell Carcinoma Thomas Jefferson University December 2019 Phase 2
NCT03854032 Not yet recruiting Lip|Oral Cavity Squamous Cell Carcinoma|Pharynx|Larynx|Squamous Cell Carcinoma Thomas Jefferson University December 2019 Phase 2
NCT03792750 Recruiting Advanced Cancer Bristol-Myers Squibb January 2 2019 Phase 1|Phase 2
NCT03792750 Recruiting Advanced Cancer Bristol-Myers Squibb January 2 2019 Phase 1|Phase 2
NCT03695250 Recruiting Metastatic Hepatocellular Carcinoma|Stage III Hepatocellular Carcinoma AJCC v8|Stage IIIA Hepatocellular Carcinoma AJCC v8|Stage IIIB Hepatocellular Carcinoma AJCC v8|Stage IV Hepatocellular Carcinoma AJCC v8|Stage IVA Hepatocellular Carcinoma AJCC v8|Stage IVB Hepatocellular Carcinoma AJCC v8|Unresectable Hepatocellular Carcinoma Edward Kim|Bristol-Myers Squibb|National Cancer Institute (NCI)|University of California Davis October 16 2018 Phase 1|Phase 2
NCT03661320 Recruiting Bladder Cancer|Muscle-Invasive Bladder Cancer|BMS-986205 Bristol-Myers Squibb October 12 2018 Phase 3

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID