Description In vitro In vivo
ChemicalBook > CAS DataBase List > indoleaMine-2,3-dioxygenase inhibitor INCB024360

indoleaMine-2,3-dioxygenase inhibitor INCB024360

Description In vitro In vivo
Product Name
indoleaMine-2,3-dioxygenase inhibitor INCB024360
CAS No.
914471-09-3
Chemical Name
indoleaMine-2,3-dioxygenase inhibitor INCB024360
Synonyms
IDO5L;CS-1034;IDO-IN-2;INCB14943;INCB024360;INCB-24360;INCB 024360;INCB-024360;IDO inhibitor;4-diaminobutane
CBNumber
CB22666639
Molecular Formula
C9H7ClFN5O2
Formula Weight
271.64
MOL File
914471-09-3.mol
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indoleaMine-2,3-dioxygenase inhibitor INCB024360 Property

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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.38256
Product name
IDO Inhibitor
Packaging
10MG
Price
$190
Updated
2024/03/01
Cayman Chemical
Product number
18265
Product name
INCB024360 analog
Purity
≥98%
Packaging
5mg
Price
$66
Updated
2024/03/01
Cayman Chemical
Product number
18265
Product name
INCB024360 analog
Purity
≥98%
Packaging
1mg
Price
$25
Updated
2021/12/16
Cayman Chemical
Product number
18265
Product name
INCB024360 analog
Purity
≥98%
Packaging
10mg
Price
$117
Updated
2024/03/01
Cayman Chemical
Product number
18265
Product name
INCB024360 analog
Purity
≥98%
Packaging
25mg
Price
$259
Updated
2024/03/01
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indoleaMine-2,3-dioxygenase inhibitor INCB024360 Chemical Properties,Usage,Production

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 INCB024360 Preparation Products And Raw materials

Raw materials

Preparation Products

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indoleaMine-2,3-dioxygenase inhibitor INCB024360 Suppliers

China 108 Germany 1 India 2 United Kingdom 1 United States 19 Global 131
Shanghai Boyle Chemical Co., Ltd.
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86-21-57758967
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sales@boylechem.com
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China
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J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
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86-10-82849933
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jkinfo@jkchemical.com
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China
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Chembest Research Laboratories Limited
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021-20908456
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021-58180499
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sales@BioChemBest.com
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Nanjing Chemlin Chemical Co., Ltd
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025-83697070
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+86-25-83453306
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Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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Shanghai Topbiochem Technology Co., Ltd
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021-58170097
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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Shanghai Aladdin Bio-Chem Technology Co.,LTD
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400-6206333 18521732826;
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021-50323701
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market@aladdin-e.com
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Moltt Biocem Co., Ltd.
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+86-21-38682181 15900741819
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+86-21-38682181
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China
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Shanghai Witofly Chemical Co.,Ltd
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sales@witofly.com
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View Lastest Price from indoleaMine-2,3-dioxygenase inhibitor INCB024360 manufacturers

Shaanxi Dideu Medichem Co. Ltd
Product
INCB024360 914471-09-3
Price
US $0.00-0.00/KG
Min. Order
5mg
Purity
99%
Supply Ability
2000tons
Release date
2019-12-31
Zhuozhou Wenxi import and Export Co., Ltd
Product
IDO5L 914471-09-3
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-06-26
Career Henan Chemical Co
Product
indoleaMine-2,3-dioxygenase inhibitor INCB024360 914471-09-3
Price
US $8.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
10tons
Release date
2018-12-24

914471-09-3, indoleaMine-2,3-dioxygenase inhibitor INCB024360Related Search:

AZD6738 SGC707 MS023 2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione 3,4-dimethoxy-N-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]benzenesulfonamide Enasidenib Epacadostat (INCB024360) LLY-507 4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide DBeQ Selumetinib Saracatinib 4-[6-[4-(1-Methylethoxy)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline Pomalidomide NLG919 AZD-9291 1-METHYL-D-TRYPTOPHAN IDO-IN-3

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  • (4E)-4-[(3-chloro-4-fluoroanilino)-nitrosomethylidene]-1,2,5-oxadiazol-3-amine
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  • INCB-24360
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  • INCB024360/INCB-024360
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  • 4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide INCB024360
  • IDO-IN-2
  • INCB024360 analogue
  • (E)-4-Amino-N'-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide
  • IDO5L
  • INCB024360 analog
  • IDO inhibitor
  • INCB024360 ANALOGUE;IDO5L
  • INCB024360 500MG
  • IDO-IN-2(1g 2000)
  • INCB024360-analog(IDO-IN-2)
  • 1,2,5-Oxadiazole-3-carboximidamide, 4-amino-N'-(3-chloro-4-fluorophenyl)-N-hydroxy-
  • indoleaMine-2,3-dioxygenase inhibitor INCB024360 USP/EP/BP
  • 4-diaminobutane
  • N-(3-Aminopropyl)-1
  • N-(4-Aminobutyl)-1
  • 4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboxamidine
  • 4-Amino-N'-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide
  • 914471-09-3
  • C9H7ClFN5O2
  • Inhibitors