indoleaMine-2,3-dioxygenase inhibitor INCB024360

Bezeichnung:indoleaMine-2,3-dioxygenase inhibitor INCB024360

CAS-Nr914471-09-3

Englisch Name:indoleaMine-2,3-dioxygenase inhibitor INCB024360

CBNumberCB22666639

SummenformelC9H7ClFN5O2

Molgewicht271.64

MOL-Datei914471-09-3.mol

indoleaMine-2,3-dioxygenase inhibitor INCB024360 physikalisch-chemischer Eigenschaften

Siedepunkt	504.7±60.0 °C(Predicted)
Dichte	1.78±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	≥13.55 mg/mL in DMSO
pka	7.54±0.69(Predicted)
Aggregatzustand	Solid
Farbe	Off-white to yellow

Gefahreninformationscode (GHS)

indoleaMine-2,3-dioxygenase inhibitor INCB024360 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
INCB024360 acts as a competitive inhibitor of (IDO1) indoleamine 2,3-dioxygenase showing effect in mouse melanoma models. IC50 = 67 nM
Biologische Aktivität
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].
Lager
Store at -20°C
Einzelnachweise
[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.

indoleaMine-2,3-dioxygenase inhibitor INCB024360 Upstream-Materialien And Downstream Produkte

indoleaMine-2,3-dioxygenase inhibitor INCB024360 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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