Home Cart Sign in  
Chemical Structure| 1204669-58-8 Chemical Structure| 1204669-58-8

Structure of Epacadostat
CAS No.: 1204669-58-8

Chemical Structure| 1204669-58-8

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.

Synonyms: INCB 024360

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

DE Stock

US Stock

Asia Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Product Citations

Feng, Xi ; Shen, Pei ; Wang, Yinuo ; Li, Zhiyu ; Bian, Jinlei ;

Abstract: Targeting Trp-Kyn pathways has been identified as an attractive approach for the cancer immunotherapies. In this study, a novel phosphonamidate containing compound was designed, synthesized and evaluated for its inhibitory activity against key dioxygenases in Trp-Kyn pathway, including IDO1, IDO2 and TDO. This compound showed potent IDO1 inhibitory activity with an IC50 value of 94 nM in an enzymatic assay and 12.6 nM in HeLa cells. In addition, this compound showed promising IDO2 inhibition and TDO inhibition with IC50 values of 310 nM and 2.6 μM, respectively, in enzyme assay. Based on the promising enzyme inhibitory activity toward IDO/TDO, compound F04 was evaluated of its antitumor effects in two tumor models. Further evaluation of mechanism demonstrated compound F04 with the remarkable capacity of reducing kynurenine level in plasma/TME and restoring anti-tumor immune response. F04 could be further developed as a potential immunotherapeutic agent combined with immune checkpoint inhibitors or chemotherapeutic drugs for cancer treatment.

Keywords: IDO1 inhibitors ; Trp-Kyn ; Phosphonamidate ; Epacadostat ; NSCLC

Purchased from AmBeed:

Alternative Products

Product Details of Epacadostat

CAS No. :1204669-58-8
Formula : C11H13BrFN7O4S
M.W : 438.23
SMILES Code : O=S(NCCNC1=NON=C1/C(NC2=CC=C(F)C(Br)=C2)=N/O)(N)=O
Synonyms :
INCB 024360
MDL No. :MFCD26142934
InChI Key :FBKMWOJEPMPVTQ-UHFFFAOYSA-N
Pubchem ID :135564890

Safety of Epacadostat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03471286 Solid Tumor PHASE1 TERMINATED 2021-07-30 Sidney Kimmel Comprehensive Ca... More >>ncer Center at Johns Hopkins, Baltimore, Maryland, 21231, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.41mL

2.28mL

1.14mL

22.82mL

4.56mL

2.28mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories