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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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]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells MljiSpVv[3Srb36gZZN{[Xl? NGXJd|lKdmirYnn0bY9vKG:oIHnu[I9t\WGvaX7lJFItOy2maX;4fYdmdmG|ZTDpckBKTk5vZ3HtcYEue3SrbYXsZZRm\CCqdX3hckBJ\UyjIHPlcIx{KGG|c3Xzd4VlKGG|IHv5cpVz\W6rbnWg[o9zdWG2aX;uJIJ6KHOyZXP0do9xcG:2b33leJJ6NCCLQ{WwQVE6KG6P M1vCNVE6PTB5OE[y
mouse B16 cells NH\3Nm9HfW6ldHnvckBie3OjeR?= MWfJcohq[mm2aX;uJI9nKGmwZH;s[YFucW6nIEKsN{1lcW:6eXflcoF{\SCrbjDtc5V{\SCEMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgb5lvfXKnbnnu[UBnd3KvYYTpc44h[nlic4DlZ5Rzd3Cqb4TvcYV1enluIFnDOVA:PDZibl2= M1n6NVE6PTB5OE[y
mouse P815B clone-6 cells NU\UUWllTnWwY4Tpc44h[XO|YYm= NGXKWG9KdmirYnn0bY9vKG:oIHj1cYFvKEmGT{GgeJJidnOoZXP0[YQhcW5ibX;1d4UhWDhzNVKgZ4xwdmVvNjDj[YxteyCkeTDIVGxEKGGwYXz5d4l{NCCLQ{WwQVYxKG6P M3zYRVIzPjF4OUCy
P815 clone 6 cells MnXNSpVv[3Srb36gZZN{[Xl? M3f6N2lvcGmkaYTpc44hd2ZibX;1d4UhUUSRMTDpckBRQDF3IHPsc45mKDZiY3XscJMh[nliSGDMR{BidmGueYPpd{whUUN3ME2wMlEh|ryP NXiyfnFOOjJ4MU[5NFI>
HEK293 clone 6 cells MXLGeY5kfGmxbjDhd5NigQ>? MkjGTY5pcWKrdHnvckBw\iCqdX3hckBKTE9zIITyZY5{\mWldHXkJIlvKEiHS{K5N{BkdG:wZTC2JINmdGy|IHL5JGhRVENiYX7hcJl{cXN? M13iclIzPjF4OUCy

... Click to View More Cell Line Experimental Data

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:[1]
+ 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 warmed (198.79 mM)
Ethanol 54 mg/mL warmed (198.79 mM)
Water Insoluble
In vivo Add solvents individually and in order:
5% DMSO+45% PEG 300+ddH2O
22mg/mL

* 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
Synonyms N/A

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02862457 Recruiting Neoplasms Merck Sharp & Dohme Corp. August 2016 Phase 1
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 Tumor|Lymphoma, Large B-Cell, Diffuse|Carcinoma, Non-Small-Cell Lung|Transitional Cell Carcinoma of Urinary Tract|Triple Negative Breast Cancer|Carcinoma, Squamous Cell of Head and Neck|Ovarian Neoplasms|Adenocarcinoma of the Endometrium|Renal Cell Carcinoma|Microsatellite-instability (MSI) High Colorectal Cancer Incyte Corporation|Merck Sharp & Dohme Corp. June 2014 Phase 1|Phase 2
NCT02118285 Suspended Ovarian Cancer|Fallopian Tube Carcinoma|Primary Peritoneal Carcinoma Masonic Cancer Center, University of Minnesota|Incyte Corporation April 2014 Phase 1

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