product name Epacadostat (INCB024360)
Description: Epacadostat, also known as INCB024360 or INCB24360, is an orally available, potent and selective IDO1 inhibitor with IC50 of 10 nM. Epacadostat has potential immunomodulating and antineoplastic activities. By inhibiting IDO1 and decreasing kynurenine in tumor cells, Epacadostat increases and restores the proliferation and activation of various immune cells, including dendritic cells, NK cells, T-cells, and a reduction in tumor-associated regulatory T cells.
References: Blood. 2010 Apr 29;115(17):3520-30; Mol Cancer Ther. 2010 Feb;9(2):489-98.
438.23
Formula
C11H13BrFN7O4S
CAS No.
1204669-58-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 87 mg/mL (198.5 mM)
Water: <1 mg/mL
Ethanol: 53 mg/mL (120.9 mM)
Solubility (In vivo)
10%DMSO+90%PEG400: 30mg/mL
Synonyms
INCB024360 or INCB24360
other peoduct :
| In Vitro |
In vitro activity: In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. Kinase Assay: Cell Assay: In Hela cells, INCB024360 selectively inhibits the activity of human IDO1 with IC50 values of about 10nM. On the other hand INCB024360demonstrates little inhibition activity against human IDO1 or TDO (tryptophan 2, 3-dioxygenase). In coculture systems of human dendritic cells with allogeneic lymphocytes, INCB024360 inhibit T-cell proliferation and cytokine production and influence the viability of NK cells. INCB024360 also increase CD86 expression and promote activation T cells by DCs. |
|---|---|
| In Vivo | INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. |
| Animal model | Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors |
| Formulation & Dosage | Dissolved in 3% N,N–Dimethylacetamide, 10% (2-Hydroxypropyl) β-Cyclodextrin; 100 mg/kg; p.o. administration |
| References | Blood. 2010 Apr 29;115(17):3520-30; Mol Cancer Ther. 2010 Feb;9(2):489-98 |
