INCB024360 analogue

Catalog No.S7587

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

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INCB024360 analogue Chemical Structure

INCB024360 analogue Chemical Structure
Molecular Weight: 271.64

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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]
IC50 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

IDO enzyme assays Human IDO with an N-terminal His tag is expressed in E.coli and purified to homogeneity. IDO catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays are performed at room temperature using 20 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 3.5 μM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates are recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine.

Animal Study: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Yue EW, et al. J Med Chem. 2009, 52(23), 7364-7367.

[2] Liu X, et al. Blood. 2010, 115(17), 3520-3530.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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|Tr  ...more 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 Neg  ...more 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 Cor  ...more Masonic Cancer Center, University of Minnesota|Incyte Corporation April 2014 Phase 1

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Chemical Information

Download INCB024360 analogue SDF
Molecular Weight (MW) 271.64
Formula

C9H7ClFN5O2

CAS No. 914471-09-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 54 mg/mL warming (198.79 mM)
Ethanol 54 mg/mL warming (198.79 mM)
Water <1 mg/mL (<1 mM)
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 Name (4E)-4-[(3-chloro-4-fluoroanilino)-nitrosomethylidene]-1,2,5-oxadiazol-3-amine

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.

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