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| 5mg |
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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. 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.
| 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].
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| 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].
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| 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 |
| Molecular Formula |
C11H13BRFN7O4S
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| Molecular Weight |
438.23
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| CAS # |
1204669-58-8
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| Related CAS # |
1204669-58-8 (INCB024360);1204669-37-3 (INCB024360);914471-09-3 (INCB14943);
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| SMILES |
O=S(NCCNC1=NON=C1/C(NC2=CC=C(F)C(Br)=C2)=N/O)(N)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.62 mg/mL (5.98 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.62 mg/mL (5.98 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: 10%DMSO+90%PEG400: 30mg/mL |
| 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.
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03361865 | Completed Has Results | Drug: Pembrolizumab Drug: Epacadostat |
UC (Urothelial Cancer) | Incyte Corporation | December 4, 2017 | Phase 3 |
| NCT03374488 | Completed Has Results | Drug: Pembrolizumab Drug: Epacadostat |
UC (Urothelial Cancer) | Incyte Corporation | December 22, 2017 | Phase 3 |
| NCT03182894 | Withdrawn | Drug: Epacadostat (INCB024360) in Combination with Pembrolizumab (MK-3475) and Azacitidine (VIDAZA) |
Metastatic Colorectal Cancer | James J Lee | September 30, 2018 | Phase 1 Phase 2 |
| NCT03516708 | Recruiting | Drug: Epacadostat Radiation: Short-course radiation |
Rectal Cancer | Washington University School of Medicine |
October 10, 2019 | Phase 1 Phase 2 |
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