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
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
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.
N-Bromosuccinimide Price
- Product number
- 5.38256
- Product name
- IDO Inhibitor
- Packaging
- 10MG
- Price
- $190
- Updated
- 2024/03/01
- Product number
- 18265
- Product name
- INCB024360 analog
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $66
- Updated
- 2024/03/01
- Product number
- 18265
- Product name
- INCB024360 analog
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $25
- Updated
- 2021/12/16
- Product number
- 18265
- Product name
- INCB024360 analog
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $117
- Updated
- 2024/03/01
- Product number
- 18265
- Product name
- INCB024360 analog
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $259
- Updated
- 2024/03/01
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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View Lastest Price from indoleaMine-2,3-dioxygenase inhibitor INCB024360 manufacturers
- 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
- 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
- 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