Linrodostat (BMS-986205)

Catalog No.S8629 Batch:S862901

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Technical Data

Formula

C24H24ClFN2O
Molecular Weight 410.91 CAS No. 1923833-60-6
Solubility (25°C)* In vitro DMSO 82 mg/mL (199.55 mM)
Ethanol 82 mg/mL (199.55 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.05mg/ml 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 95% Corn oil
2.05mg/ml 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. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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)

Selleck's Linrodostat (BMS-986205) has been cited by 6 publications

YH29407 with anti-PD-1 ameliorates anti-tumor effects via increased T cell functionality and antigen presenting machinery in the tumor microenvironment [ Front Chem, 2022, 10:998013] PubMed: 36545214
IDO Inhibition Facilitates Antitumor Immunity of Vγ9Vδ2 T Cells in Triple-Negative Breast Cancer [ Front Oncol, 2021, 11:679517] PubMed: 34381711
Decreased IDO1 Dependent Tryptophan Metabolism in Aged Lung during Influenza [ Eur Respir J, 2020, 2000443] PubMed: 33243840
Prognostic value of indoleamine 2,3 dioxygenase in patients with higher-risk myelodysplastic syndromes treated with azacytidine [ Br J Haematol, 2020, 190(3):361-370] PubMed: 32350858
Prognostic value of indoleamine 2,3 dioxygenase in patients with higher-risk myelodysplastic syndromes treated with azacytidine [ Br J Haematol, 2020, 190(3):361-370] PubMed: 32350858
Displacement Induced Off-On Fluorescent Biosensor Targeting IDO1 Activity in Live Cells. [ Anal Chem, 2019, 91(23):14943-14950] PubMed: 31714063

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.