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indoleaMine-2,3-dioxygenase inhibitor INCB024360

Basic information Description In vitro In vivo Safety Supplier Related

indoleaMine-2,3-dioxygenase inhibitor INCB024360 Basic information

Product Name:
indoleaMine-2,3-dioxygenase inhibitor INCB024360
Synonyms:
  • CS-1034
  • Epacadostat-analog
  • INCB14943
  • INCB024360 analogue(IDO-IN-1)
  • 3-dioxygenase inhibitor INCB024360
  • INCB-024360; INCB 024360; INCB-24360; INDOLEAMINE-2;3-DIOXYGENASE INHIBITOR INCB024360
  • indoleaMine-2,3-dioxygenase inhibitor
  • INCB 024360-analog - IDO inhibitor 5l
CAS:
914471-09-3
MF:
C9H7ClFN5O2
MW:
271.64
Product Categories:
  • Inhibitors
Mol File:
914471-09-3.mol
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indoleaMine-2,3-dioxygenase inhibitor INCB024360 Chemical Properties

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
pka
7.54±0.69(Predicted)
form 
Solid
color 
Off-white to yellow
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indoleaMine-2,3-dioxygenase inhibitor INCB024360 Usage And Synthesis

Description

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).

In vitro

In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells.

In vivo

INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine.

Uses

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

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.

indoleaMine-2,3-dioxygenase inhibitor INCB024360Supplier

Shanghai Boyle Chemical Co., Ltd.
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sales@boylechem.com
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Product Name:INCB024360
CAS:914471-09-3
J & K SCIENTIFIC LTD.
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Product Name:INCB024360
CAS:914471-09-3
Package:100Mg,25Mg,50Mg
Chembest Research Laboratories Limited
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Product Name:INCB024360 analogue
CAS:914471-09-3
Purity:98%+ Package:50mg;100mg;500mg;1g;5g;10g
BeiJing Hwrk Chemicals Limted
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Product Name:4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3 -carboximidamide
CAS:914471-09-3
Purity:98.00% Package:1g
Nanjing Chemlin Chemical Co., Ltd
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Product Name:4-Amino-N'-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide
CAS:914471-09-3
Purity:98% Package:5KG; 1KG