INCB024360 (Epacadostat), IDO Inhibitor


Catalog No. size PriceQuantity
M60292-2S 2 mg solid $109
M60292-10S 10 mg solid $431

Description

INCB024360 is a potent and selective indoleamine 2, 3-dioxygenase (IDO1) inhibitor with IC50 ~10 nM It displays high selectivity over other related enzymes such as IDO2 or tryptophan 2, 3-dioxygenase (TDO). In coculture systems of human allogeneic lymphocytes with dendritic cells (DCs) or tumor cells, INCB024360 inhibition of IDO1 promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. Administration of INCB024360 to tumor-bearing mice significantly inhibits tumor growth in a lymphocyte-dependent manner. INCB024360 has completed Phase I clinical trials and is now being used in combination with other cancer immunotherapy agents.

Product information

CAS Number: 1204669-58-8

Molecular Weight: 438.23

Formula: C11H13BrFN7O4S

Chemical Name: (Z)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-(2-(sulfamoylamino)ethylamino)-1, 2, 5-oxadiazole-3-carboximidamide

Smiles: NS(=O)(=O)NCCNC1=NON=C1/C(/NC1=CC(Br)=C(F)C=C1)=N/O

InChiKey: FBKMWOJEPMPVTQ-UHFFFAOYSA-N

InChi: InChI=1S/C11H13BrFN7O4S/c12-7-5-6(1-2-8(7)13)17-11(18-21)9-10(20-24-19-9)15-3-4-16-25(14,22)23/h1-2,5,16,21H,3-4H2,(H,15,20)(H,17,18)(H2,14,22,23)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

INCB024360 was used at 1 µM final concentration in various in vitro assays.

In Vivo:

INCB024360 was dosed at 75 mg/Kg (BID, subcutaneous injection) to mice bearing GM-CSF-secreting B16 tumors. Formulation is 5% DMA, 47.5% propylene glycol.

References:

  1. Yue EW, et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. (2009) J Med Chem. 52(23):7364-7.
  2. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. (2010) Blood. 115(17):3520-30.

Products are for research use only. Not for human use.

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