INCB024360 analogue

Catalog No.S7587

INCB024360 analogue Chemical Structure

Molecular Weight(MW): 271.64

INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Phase 2.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Phase 2.
Targets
IDO1 [1]
67 nM
In vitro

In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 nM. [1] In coculture systems of human allogeneic lymphocytes with dendritic cells or tumor cells, INCB024360, via IDO1 inhibition, reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs, and increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells. [2]

In vivo In mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. [1] INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice. [2]

Protocol

Animal Research
+ Expand
  • Animal Models: Mice bearing GM-CSF-secreting B16 tumors
  • Formulation: 5% DMA, 47.5% propylene glycol
  • Dosages: 75 mg/kg b.i.d
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 54 mg/mL (198.79 mM) warming
Ethanol 54 mg/mL warmed (198.79 mM)
Water <1 mg/mL
In vivo 2% DMSO+corn oil 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 271.64
Formula

C9H7ClFN5O2

CAS No. 914471-09-3
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02785250 Recruiting Recurrent Epithelial Ovarian Cancer|Recurrent Fallopian Tube Cancer|Recurrent Peritoneal Cancer ImmunoVaccine Technologies, Inc.|Incyte Corporation April 2016 Phase 1
NCT02575807 Recruiting Platinum-resistant Ovarian Cancer|Platinum-resistant Fallopian Cancer|Platinum-resistant Peritoneal Cancer Aduro Biotech, Inc.|Incyte Corporation January 2016 Phase 1|Phase 2
NCT02318277 Recruiting Selected Advanced Solid Tumors|Non-small Cell Lung Cancer|Melanoma|Head and Neck Cancer|Gastric Cancer|Gastroesophageal Cancer|Urothelial Cancer|Triple Negative Breast Cancer Incyte Corporation|MedImmune LLC December 2014 Phase 1|Phase 2
NCT02178722 Recruiting Malignant Solid Tumour|Lymphoma, Large B-Cell, Diffuse|Carcinoma, Non-Small-Cell Lung|Transitional Cell Carcinoma of Genitourinary Tract|Triple Negative Breast Cancer|Carcinoma, Squamous Cell of Head and Neck|Ovarian Neoplasms|Adenocarcinoma of the Endometrium|Renal Cell Carcinoma Incyte Corporation|Merck Sharp & Dohme Corp. June 2014 Phase 1|Phase 2
NCT02118285 Recruiting Ovarian Cancer|Fallopian Tube Carcinoma|Primary Peritoneal Carcinoma Masonic Cancer Center, University of Minnesota|Incyte Corporation April 2014 Phase 1
NCT01982487 Withdrawn Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer|Stage IA Fallopian Tube Cancer|Stage IA Ovarian Epithelial Cancer|Stage IA Primary Peritoneal Cavity Cancer|Stage IB Fallopian Tube Cancer|Stage IB Ovarian Epithelial Cancer|Stage IB Primary Peritoneal Cavity Cancer|Stage IC Fallopian Tube Cancer|Stage IC Ovarian Epithelial Cancer|Stage IC Primary Peritoneal Cavity Cancer|Stage IIA Fallopian Tube Cancer|Stage IIA Ovarian Epithelial Cancer|Stage IIA Primary Peritoneal Cavity Cancer|Stage IIB Fallopian Tube Cancer|Stage IIB Ovarian Epithelial Cancer|Stage IIB Primary Peritoneal Cavity Cancer|Stage IIC Fallopian Tube Cancer|Stage IIC Ovarian Epithelial Cancer|Stage IIC Primary Peritoneal Cavity Cancer|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Epithelial Cancer|Stage IIIA Primary Peritoneal Cavity Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Epithelial Cancer|Stage IIIB Primary Peritoneal Cavity Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Epithelial Cancer|Stage IIIC Primary Peritoneal Cavity Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Epithelial Cancer|Stage IV Primary Peritoneal Cavity Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI) December 2013 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID