ChemicalBook >> CAS DataBase List >>indoleaMine-2,3-dioxygenase inhibitor INCB024360

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
Molecular Weight:
271.64
MDL Number:
MFCD28142835
MOL File:
914471-09-3.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59

indoleaMine-2,3-dioxygenase inhibitor INCB024360 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
FDA UNII 2HR315841W

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338
NFPA 704
0
2 0

indoleaMine-2,3-dioxygenase inhibitor INCB024360 price More Price(28)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 5.38256 IDO Inhibitor 10MG $190 2024-03-01 Buy
Cayman Chemical 18265 INCB024360 analog ≥98% 914471-09-3 5mg $66 2024-03-01 Buy
Cayman Chemical 18265 INCB024360 analog ≥98% 914471-09-3 1mg $25 2021-12-16 Buy
Cayman Chemical 18265 INCB024360 analog ≥98% 914471-09-3 10mg $117 2024-03-01 Buy
Cayman Chemical 18265 INCB024360 analog ≥98% 914471-09-3 25mg $259 2024-03-01 Buy
Product number Packaging Price Buy
5.38256 10MG $190 Buy
18265 5mg $66 Buy
18265 1mg $25 Buy
18265 10mg $117 Buy
18265 25mg $259 Buy

indoleaMine-2,3-dioxygenase inhibitor INCB024360 Chemical Properties,Uses,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.

372-19-0
147085-13-0
914471-09-3
Synthesis of indoleaMine-2,3-dioxygenase inhibitor INCB024360 from 3-Fluoroaniline and 1,2,5-Oxadiazole-3-carboxiMidoyl chloride, 4-aMino-N-hydroxy-

indoleaMine-2,3-dioxygenase inhibitor INCB024360 Preparation Products And Raw materials

Global( 130)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29914 58
Zhejiang ZETian Fine Chemicals Co. LTD
18957127338 stella@zetchem.com China 2141 58
Biochempartner
0086-13720134139 candy@biochempartner.com CHINA 967 58
Hubei xin bonus chemical co. LTD
86-13657291602 linda@hubeijusheng.com CHINA 22968 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
Shaanxi Dideu Medichem Co. Ltd
+86-29-87569265 +86-18612256290 1056@dideu.com China 3791 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
WinWin Chemical CO., Limited
+86-0086-577-64498589 +86-15355981851 sales@win-winchemical.com China 13854 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250 1026@dideu.com China 29474 58

View Lastest Price from indoleaMine-2,3-dioxygenase inhibitor INCB024360 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
INCB024360 pictures 2021-07-20 INCB024360
914471-09-3
US $0.00-0.00 / KG 5mg 99% 2000tons Shaanxi Dideu Medichem Co. Ltd
IDO5L pictures 2021-07-02 IDO5L
914471-09-3
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
indoleaMine-2,3-dioxygenase inhibitor INCB024360 pictures 2019-07-06 indoleaMine-2,3-dioxygenase inhibitor INCB024360
914471-09-3
US $8.00 / kg 1kg 99% 10tons Career Henan Chemical Co
  • INCB024360 pictures
  • INCB024360
    914471-09-3
  • US $0.00-0.00 / KG
  • 99%
  • Shaanxi Dideu Medichem Co. Ltd
  • IDO5L pictures
  • IDO5L
    914471-09-3
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd

indoleaMine-2,3-dioxygenase inhibitor INCB024360 Spectrum

(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) N-(4-Aminobutyl)-1 N-(3-Aminopropyl)-1 4-diaminobutane indoleaMine-2,3-dioxygenase inhibitor INCB024360 USP/EP/BP 1,2,5-Oxadiazole-3-carboximidamide, 4-amino-N'-(3-chloro-4-fluorophenyl)-N-hydroxy- INCB024360-analog(IDO-IN-2) INCB 024360-analog - IDO inhibitor 5l indoleaMine-2,3-dioxygenase inhibitor INCB-024360; INCB 024360; INCB-24360; INDOLEAMINE-2;3-DIOXYGENASE INHIBITOR INCB024360 3-dioxygenase inhibitor INCB024360 INCB024360 analogue(IDO-IN-1) INCB14943 Epacadostat-analog CS-1034 4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboxamidine 914471-09-3 C9H7ClFN5O2 Inhibitors