INCB024360 analogue

Catalog No.S7587 Synonyms: INCB14943

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.

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Biological Activity

Description INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM.
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 MkO4SpVv[3Srb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKGmwZH;s[YFucW6nIEKsN{1lcW:6eXflcoF{\SCrbjDJSm4u\2GvbXGtd5RqdXWuYYTl[EBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGu7boXy[Y5qdmViZn;ycYF1cW:wIHL5JJNx\WO2cn;wbI91d22ndIL5MEBKSzVyPUG5JI5O NIO4R4IyQTVyN{i2Ni=>
mouse B16 cells MVTGeY5kfGmxbjDhd5NigQ>? NG[3NXpKdmirYnn0bY9vKG:oIHnu[I9t\WGvaX7lJFItOy2maX;4fYdmdmG|ZTDpckBud3W|ZTDCNVYh[2WubIOgZZN{\XO|ZXSgZZMhc3mwdYLlcolv\SCob4LtZZRqd25iYomgd5Bm[3S{b4Doc5RwdWW2comsJGlEPTB;NE[gcm0> M1XvZVE6PTB5OE[y
mouse P815B clone-6 cells NETIOYNHfW6ldHnvckBie3OjeR?= MojiTY5pcWKrdHnvckBw\iCqdX3hckBKTE9zIITyZY5{\mWldHXkJIlvKG2xdYPlJHA5OTWEIHPsc45mNTZiY3XscJMh[nliSGDMR{BidmGueYPpd{whUUN3ME22NEBvVQ>? NE\3TVAzOjZzNkmwNi=>
P815 clone 6 cells NFTWXFJHfW6ldHnvckBie3OjeR?= MlW5TY5pcWKrdHnvckBw\iCvb4Xz[UBKTE9zIHnuJHA5OTViY3zvcoUhPiClZXzsd{BjgSCKUFzDJIFv[Wy7c3nzMEBKSzVyPUCuNUDPxE1? MXeyNlYyPjlyMh?=
HEK293 clone 6 cells NV;4bGpCTnWwY4Tpc44h[XO|YYm= M4rsTWlvcGmkaYTpc44hd2ZiaIXtZY4hUUSRMTD0doFve2[nY4Tl[EBqdiCKRVuyPVMh[2yxbnWgOkBk\WyuczDifUBJWEyFIHHuZYx6e2m| M1zs[FIzPjF4OUCy

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
NMNAT2; 

PubMed: 28266613     


Western blots show NMNAT2 and GAPDH levels in DIV14 cortical neurons after 6 hrs of treatment with 8-Bromo-cAMP, caffeine or Bay-K.

28266613
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]

- Collapse
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.
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
in solvent
Synonyms INCB14943

Bio Calculators

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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