- INCB-24360;INCB24360
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- $15.00 / 1KG
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2021-07-13
- CAS:1204669-58-8
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
- Epacadostat (INCB024360)
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- $6.68 / 1KG
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2020-01-09
- CAS:1204669-58-8
- Min. Order: 1KG
- Purity: 97%-99%
- Supply Ability: 1kg-1000kg
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| | Epacadostat (INCB024360) Basic information |
| Product Name: | Epacadostat (INCB024360) | | Synonyms: | (Z)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-((2-(sulfamoylamino)ethyl)amino)-1,2,5-oxadiazole-3-carboximidamide;Epacadostat (INCB24360, INCB024360);N-(3-Bromo-4-fluoro-phenyl)-N'-hydroxy-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole-3-carboxamidine;INCN024360;(Z)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole-3-carboxamidine;Epacadostat(INCN024360);INCB-24360(INCB-024360);Epacadostat(INCB024360) | | CAS: | 1204669-58-8 | | MF: | C11H13BrFN7O4S | | MW: | 438.23 | | EINECS: | | | Product Categories: | | | Mol File: | 1204669-58-8.mol |  |
| | Epacadostat (INCB024360) Chemical Properties |
| Melting point | 159 - 161°C | | Boiling point | 700.9±70.0 °C(Predicted) | | density | 2.01±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to at least 25 mg/ml) | | form | solid | | pka | 7.65±0.69(Predicted) | | color | White | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| | Epacadostat (INCB024360) Usage And Synthesis |
| Description | Epacadostat is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with an IC50 value of 7.1 nM in HeLa cells that demonstrates little activity against the related enzymes IDO2 or tryptophan 2,3-dioxygenase (TDO). It has been shown to promote T and natural killer-cell growth, to increase IFN-γ production, and to reduce conversion to regulatory T (Treg)-like cells in a coculture system of human allogeneic lymphocytes with either dendritic cells or tumor cells. Epacadostat can also inhibit tumor growth in tumor-bearing mice in a lymphocyte-dependent manner. | | Uses | Epacadostat is a potent and novel indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. It has high selectivity over IDO2 and tryptophan 2,3-dioxygenase (TDO). | | target | IDO1 | | References | 1) Liu?et al.?(2010),?Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity;?Blood?115?3520
2) Koblish?et al.?(2010),?Hydroxyamidine Inhibitors of Indolamine-2,3-dioxygenase Potently Suppress Systemic Tryptophan Catabolism and the Growth of IDO-Expressing Tumors;?Mol. Cancer Ther.?9?489
3) Jochems?et al.?(2016),?The IDO1 selective inhibitor epacadostat enhances dendritic cell immunogenicity and lytic ability of tumor antigen-specific T cells;?Oncotarget?7?37762
4) Yentz and Smith (2018),?Indoleamine-2,3-dioxygenase Inhibition as a Strategy to Augment Cancer Immunotherapy;?BioDrugs?32?311
5) Zhu??et al.?(2019),?Indoleamine Dioxygenase Inhibitors: Clinical Rationale and Current Development;?Curr. Oncol. Rep.?21?2
6) Mitchell?et al.?(2018),?Epacadostat Plus Pembrolizumab in Patients with Advanced Solid Tumors: Phase I Results From a Multicenter, Open-Label Phase I/II Trial (ECHO-202/KEYNOTE-037);?J. Clin. Oncol.?36?3223 |
| | Epacadostat (INCB024360) Preparation Products And Raw materials |
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