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Epacadostat (INCB024360)

Epacadostat (INCB024360) structure

CAS No:
1204669-58-8
Formula:
C11H13BrFN7O4S
Chemical 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)
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Epacadostat has been used in trials studying the treatment of HL, Melanoma, Glioblastoma, Mucosal Melanoma, and Ovarian Carcinoma, among others.|Epacadostat is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. Epacadostat targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, INCB024360 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells, and T-lymphocytes, as well as interferon (IFN) production, and a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1 is overexpressed by a variety of tumor cell types and DCs.

Epacadostat (INCB024360) Basic Attributes

Molecular Weight：

438.23

Exact Mass：

436.99171

UNII：

71596A9R13

NCI Thesaurus Code：

C92582

Color/Form：

White

ATC Code：

L - Antineoplastic and immunomodulating agents

Characteristics

Density：

2.01±0.1 g/cm3(Predicted)

Melting Point：

159 - 161°C

Boiling Point：

700.9±70.0 °C(Predicted)

PKA：

7.65±0.69(Predicted)

Critical Temperature & Pressure：

-20°C

Safety Information

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P312, P322, P330, P363, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

MeSH Entry Terms：

epacadostat

Epacadostat (INCB024360) Use and Manufacturing

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).

Recommended Suppliers of Epacadostat (INCB024360)

SHANGHAI LABWELLX BIOPHARMATECH CO., LTD. Contact Supplier

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(Z)-N-(3-Bromo-4-fluorophenyl)-N'-hydroxy-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole-3-carboxamidine , Epacadostat

CAS No.: 1204669-58-8

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INCB-24360(INCB-024360)

CAS No.: 1204669-58-8

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