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Epacadostat (INCB024360)

  Cat. No.:  DC8389   Featured
Chemical Structure
1204669-58-8
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More than 5000 active chemicals with high quality for research!
Field of application
Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1204669-58-8
Chemical Name: Epacadostat
Synonyms: HY-15689;Epacadostat;INCB-24360(INCB-024360);Epacadostat (INCB024360);IDO inhibitor 1;INCB024360;INCB-024360;INCB-24360;INCB 024360;Epacadostat(INCB 024360);AK174791;71596A9R13;N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-{[2-(sulfamoylamino)ethyl]amino}-1,2,5-oxadiazole-3-carboximidamide;Epacadostat [USAN:INN];Epacadostat; INCB024360;Epacadostat (JAN/USAN/INN);GTPL8221;FBKMWOJEPMPVTQ-UHFFFAOYSA-N;INCB 24360;BDBM222999;BCP1
SMILES: BrC1=C(C([H])=C([H])C(=C1[H])/N=C(/C1C(=NON=1)N([H])C([H])([H])C([H])([H])N([H])S(N([H])[H])(=O)=O)\N([H])O[H])F
Formula: C11H13BrFN7O4S
M.Wt: 438.2328
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.
In Vivo: Female Balb/c mice bearing CT26 tumors are treated orally twice daily for 12 d with Epacadostat at 100 mg/kg. Epacadostat (INCB 024360) suppresses kynurenine equivalently in plasma, tumors, and lymph nodes. In naïve C57BL/6 mice, 50 mg/kg Epacadostat (INCB 024360) decreases plasma kynurenine levels within 1 hour and those levels stay at least 50% suppressed through the 8-hour time course[2].
In Vitro: In cellular assays, Epacadostat (INCB 024360) selectively inhibits human IDO1 with IC50 values of approximately 10 nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat (INCB 024360) also exhibits significant activity toward mouse IDO1, with an IC50 value of 52.4 nM±15.7 nM, in a similar assay using mouse IDO1-transfected HEK293/MSR cells[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC10022 PF06840003 PF-06840003 is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1),with potential immunomodulating and antineoplastic activities.
DC8021 Indoximod (NLG-8189) NLG-8189 is an inhibitor of IDO and INDOL1 (IDO2)
DC7015 INCB024360 analogue(IDO-IN-1) INCB024360 is a potent IDO1 inhibitor(IC50=10 nM) with desirable pharmaceutical properties, which is poised to start clinical trials in cancer patients.
DC10421 IDO-IN-2 IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.
DC10098 IDO-IN-1 IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM, shows activity in Hela cell (IC50=12 nM).
DC8389 Epacadostat (INCB024360) Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.
DC10131 BMS-986205(Linrodostat) BMS-986205 is an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic activity, alone and in combination with nivolumab in advanced cancers in a phase 1/2a trial
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