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
color: Off-white to yellow

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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 110 Germany 1 India 2 United Kingdom 1 United States 19 Global 133

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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

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

(4E)-4-[(3-chloro-4-fluoroanilino)-nitrosomethylidene]-1,2,5-oxadiazol-3-amine

INCB 024360

INCB024360

INCB-024360

INCB-24360

indoleaMine-2,3-dioxygenase inhibitor INCB024360

INCB024360/INCB-024360

4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide

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