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HomeProduct name listindoleaMine-2,3-dioxygenase inhibitor INCB024360

indoleaMine-2,3-dioxygenase inhibitor INCB024360

indoleaMine-2,3-dioxygenase inhibitor INCB024360 Structural

What is indoleaMine-2,3-dioxygenase inhibitor INCB024360?

The Uses of indoleaMine-2,3-dioxygenase inhibitor INCB024360

INCB024360 acts as a competitive inhibitor of (IDO1) indoleamine 2,3-dioxygenase showing effect in mouse melanoma models. IC50 = 67 nM

What are the applications of Application

INCB024360 is a competitive IDO (indoleamine 2,3-dioxygenase) inhibitor

Biological Activity

incb024360 analogue is a potent and selective inhibitor of ido1 with ic50 value of 67 nm. [1]ido (indoleamine-pyrrole 2, 3-dioxygenase) is an enzyme which is encoded by the ido1 gene. ido is the rate-limiting and first enzyme of tryptophan which is one amino acid of human catabolism through kynurenine pathway. the decrease of l-tryptophan can cause halted growth of t cells as well as microbes. ido belongs to immunomodulatory enzyme. it is produced by some activated macrophages and immunoregulatory cells. ido is overexpressed in a wide range of cancer cells such as lung, prostatic, pancreatic, colorectal cancer. it is indentified to help cancer cells to escape the immune system by reducing the level of l-tryptophan in the microenvironment of cells.[2]in hela cells, incb024360 analogue selectively inhibited the activity of human ido1 with ic50 value of 19 nm. on the other hand, incb024360 analogue demonstrated little inhibition activity against tdo (tryptophan 2, 3-dioxygenase). in murine b16 cells, incb024360 analogue inhibited ido with ic50 value of 46 nm [1].in naive c57bl/6 mice, 100 mg/kg incb024360 analogue injected subcutaneously reduced kynurenine levels by >50% via inhibition of ido activity. in c57bl/6 mice bearing gm-csf- secreting b16 tumors, incb024360 analogue (25, 50, and 75 mg/kg b.i.d.) injected subcutaneously for 14 days dose-dependently inhibited tumor growth [1].

storage

Store at -20°C

References

[1]. yue ew1, douty b, wayland b, et al. discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. j med chem. 2009 dec 10;52(23):7364-7.
[2]. uyttenhove c, pilotte l, theate i, stroobant v, colau d, parmentier n, boon t, van den eynde bj: evidence for a tumoral immune resistance mechanism based on tryptophan degradation by indoleamine 2,3-dioxygenase. nat med 2003, 9(10):1269-1274.

Properties of indoleaMine-2,3-dioxygenase inhibitor INCB024360

Boiling point: 504.7±60.0 °C(Predicted)
Density  1.78±0.1 g/cm3(Predicted)
storage temp.  Store at -20°C
solubility  ≥13.55 mg/mL in DMSO
form  Solid
pka 7.54±0.69(Predicted)
color  Off-white to yellow

Safety information for indoleaMine-2,3-dioxygenase inhibitor INCB024360

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for indoleaMine-2,3-dioxygenase inhibitor INCB024360

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