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1923833-60-6

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1923833-60-6 Usage

Biological Activity

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.

Description

BMS-986205, also known as Linrodostat, ONO-7701 and F001287, a potent and selective, orally active IDO1 inhibitor with potential immunomodulating and antineoplastic activities.

Uses

BMS-986205 is a compound being studied for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders.

Check Digit Verification of cas no

The CAS Registry Mumber 1923833-60-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,9,2,3,8,3 and 3 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1923833-60:
(9*1)+(8*9)+(7*2)+(6*3)+(5*8)+(4*3)+(3*3)+(2*6)+(1*0)=186
186 % 10 = 6
So 1923833-60-6 is a valid CAS Registry Number.

1923833-60-6Downstream Products

1923833-60-6Relevant articles and documents

Rapid Development of a Commercial Process for Linrodostat, an Indoleamine 2,3-Dioxygenase (IDO) Inhibitor

Fraunhoffer, Kenneth J.,Delmonte, Albert J.,Beutner, Gregory L.,Bultman, Michael S.,Camacho, Kathryn,Cohen, Benjamin,Dixon, Darryl D.,Fan, Yu,Fanfair, Dayne,Freitag, Adam J.,Glace, Andrew W.,Gonzalez-Bobes, Francisco,Gujjar, Manjunath,Haley, Matthew W.,Hickey, Matthew R.,Ho, Jeanne,Iyer, Vidya,Maity, Prantik,Patel, Sunil,Rosso, Victor W.,Schmidt, Michael A.,Stevens, Jason M.,Tan, Yichen,Wilbert, Christopher,Young, Ian S.,Yu, Miao

, p. 2482 - 2498 (2019)

The process development and the kilogram-scale synthesis of linrodostat (BMS-986205, 1) are described. The synthesis features several highly efficient telescoped processes and the use of Evans auxiliary to install a methyl-bearing stereocenter. The target was prepared in 12 steps with 7 isolations in an overall yield of 31%.

IMMUNOREGULATORY AGENTS

-

, (2016/06/01)

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

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