Linrodostat is a selective and irreversible inhibitor of indoleamine 2, 3-dioxygenase 1 (IDO1) in IDO1-HeK293 cells with IC50=1.1 nM. It has good pharmacological properties in advanced cancer.

 

Brand: BCM

 

Target Activity: IDO1:1.7 nM (Cell-free)

 

In Vitro: BMS-986205 shows potent inhibition of kynurenine production in IDO1-HEK293 cells (IC50: 1.1 nM) but not in TDO-HEK293 cells[1].

 

Boiling Point: 606.8±45.0 °C(Predicted)

 

Solubility: Soluble in DMSO:25 mg/mL. Soluble in Ethanol: 15 mg/mL. Insoluble in Water.

 

Reference: 

 

1. Lillian L. Siu, et al. Abstract CT116: BMS-986205, an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic (PD) activity, alone and in combination with nivolumab (nivo) in advanced cancers in a phase 1/2a trial. AACR; Cancer Res. 2017; 77 (13 Suppl): Abstract nr CT116.

 

Attribute
[CAS No.]	1923833-60-6
[Formula]	C24H24ClFN2O
[Molecular]	410.9115632
[Chem Name]	(2R)-N-(4-chlorophenyl)-2-[4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamid
[Synonym]	Linrodostat; BMS-986205; CS-2743;
[Storage]	Sealed in dry, 2-8°C
[MDL No.]	MFCD31619233
[Form]	Powder

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