Free shipping on all orders over $ 500

Epacadostat

Cat. No. M6136
Epacadostat Structure
Synonym:

INCB024360

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
2mg USD 35  USD35 In stock
5mg USD 50  USD50 In stock
10mg USD 75  USD75 In stock
50mg USD 140  USD140 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

In vitro: 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.

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.

Protocol (for reference only)
Cell Experiment
Cell lines CEA-specific T-cell
Preparation method The IDO1 selective inhibitor epacadostat, obtained through a Cooperative Research and Development Agreement with Incyte Corporation (Wilmington, DE), was dissolved in DMSO and used at different concentrations as described. The concentration used in most experiments, 1.0 μM, was chosen to mimic the serum concentration observed in patients receiving 300 mg BID, where there was > 90% inhibition of IDO1.
Concentrations 0, 0.25 or 1.0 μM
Incubation time 48 h
Animal Experiment
Animal models Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors
Formulation 3% N,N–Dimethylacetamide, 10% (2-Hydroxypropyl) β-Cyclodextrin Dosages: ~100 mg/kg, twice a day
Dosages ~100 mg/kg, twice a day
Administration p.o.
Chemical Information
Molecular Weight 438.23
Formula C11H13BrFN7O4S
CAS Number 1204669-58-8
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jochems C, et al. Oncotarget. The IDO1 selective inhibitor epacadostat enhances dendritic cell immunogenicity and lytic ability of tumor antigen-specific T cells.

[2] Shi JG, et al. J Clin Pharmacol. Potential Underprediction of Warfarin Drug Interaction From Conventional Interaction Studies and Risk Mitigation: A Case Study With Epacadostat, an IDO1 Inhibitor.

Related IDO Products
IDO-IN-18

IDO-IN-18 is an IDO inhibitor.

IDO1-IN-21

IDO1-IN-21 is an IDO1 inhibitor (IC50 = 0.64 μM).

IDO1-IN-22

IDO1-IN-22 is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM).

IDO1/TDO-IN-6

IDO1/TDO-IN-6 is a dual inhibitor of IDO1/TDO with IC50s of 2.25 and 2.89 μM, respectively.

IDO-IN-13 

IDO-IN-13 is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an EC50 of 17 nM, extracted from patent WO2019040102A1, example 43.

  Catalog
Abmole Inhibitor Catalog




Keywords: Epacadostat, INCB024360 supplier, IDO, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.