Epacadostat (INCB024360)

Alias: INCB14943-analog; INCB-14943-analog; INCB 14943-analog;INCB024360 or INCB24360; Epacadostat-analog; IDO-IN-1;INCB 024360; INCB-024360; INCB-24360; INCB 24360;
Cat No.:V0942 Purity: ≥98%
Epacadostat (formerly INCB024360;IDO-IN-1;INCB-024360; INCB-24360; INCB24360) is an orally bioavailable, potent and selective IDO1(indoleamine-(2,3)-dioxygenase) inhibitor with potential immunomodulating and antitumor activity.
Epacadostat (INCB024360) Chemical Structure CAS No.: 1204669-58-8
Product category: IDO
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
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1g
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Other Forms of Epacadostat (INCB024360):

  • INCB024360 analogue
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's Epacadostat (INCB024360) has been cited by 2 publications
Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

Epacadostat (formerly INCB024360; IDO-IN-1; INCB-024360; INCB-24360; INCB24360) is an orally bioavailable, potent and selective IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with potential immunomodulating and antitumor activity. In inhibits IDO1 with an IC50 of 10 nM. By inhibiting IDO1 in tumor cells. Epacadostat increases and restores the proliferation and activation of various immune cells such as dendritic cells, NK cells, T-cells. Epacadostat was under investigation in a phase 3 clinical trial. But according to the results presented at the 2018 ASCO Annual Meeting, in patients with unresectable or metastatic melanoma, adding epacadostat to pembrolizumab (Keytruda) did not result in greater clinical benefit over pembrolizumab alone, according to data from the phase III ECHO-301/KEYNOTE-252 study.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Epacadostat (INCB 024360) has no effect on other related enzymes like IDO2 or tryptophan 2,3-dioxygenase (TDO), but it specifically inhibits human IDO1 in cellular experiments with an IC50 value of about 10 nM. In a comparable test utilizing mouse IDO1-transfected HEK293/MSR cells, epacadostat (INCB 024360) also shown considerable action against mouse IDO1, with an IC50 value of 52.4 nM±15.7 nM [1].
ln Vivo
For a period of 12 days, female Balb/c mice with CT26 tumors were given an oral dose of 100 mg/kg of epacadostat twice a day. Kynurenine is potently inhibited in plasma, tumors, and lymph nodes by epacadostat (INCB 024360). 50 mg/kg Epacadostat (INCB 024360) decreased plasma kynurenine levels in naive C57BL/6 mice in less than an hour, and these levels stayed at least 50% suppressed for the duration of an 8-hour period[2].
Animal Protocol

#1: Dissolved in 3% N,N–Dimethylacetamide, 10% (2-Hydroxypropyl) β-Cyclodextrin; 100 mg/kg; p.o. administration;

#2: Dissolved in 10% DMSO, 40% PEG 300, and 50% NaCl 0.9% [3]

Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors
References
[1]. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30.
[2]. Koblish HK, et al. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9(2):489-98.
[3]. Fu R, et al. LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour micro-environment. Br J Pharmacol. 2018 Jul;175(14):3034-3049
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H13BRFN7O4S
Molecular Weight
438.23
CAS #
1204669-58-8
SMILES
O=S(NCCNC1=NON=C1/C(NC2=CC=C(F)C(Br)=C2)=N/O)(N)=O
Synonyms
INCB14943-analog; INCB-14943-analog; INCB 14943-analog;INCB024360 or INCB24360; Epacadostat-analog; IDO-IN-1;INCB 024360; INCB-024360; INCB-24360; INCB 24360;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
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
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2819 mL 11.4095 mL 22.8191 mL
5 mM 0.4564 mL 2.2819 mL 4.5638 mL
10 mM 0.2282 mL 1.1410 mL 2.2819 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
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