E7046 (ER-886406)

For research use only.

Catalog No.S6649

E7046 (ER-886406) Chemical Structure

CAS No. 1369489-71-3

E7046 (ER-886406) is a selective inhibitor of the prostaglandin E2 (PGE2) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM.

Purity & Quality Control

Choose Selective Prostaglandin Receptor Inhibitors

Biological Activity

Description E7046 (ER-886406) is a selective inhibitor of the prostaglandin E2 (PGE2) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM.
Targets
EP4 [1]
(Cell-free assay)
EP4 [1]
(Cell-free assay)
13.5nM 23.14 nM(Ki)
In vitro

E7046 has specific and potent inhibitory activity on PGE2-mediated pro-tumor myeloid cell differentiation and activation.[1]

In vivo

E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8+ T cells.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: Monocytes
  • Concentrations: 10,100,300,1000,or 3000 nM
  • Incubation Time: 7d
  • Method:

    Monocytes are placed in culture with recombinant human GM-CSF (20 ng/mL) + human IL-4 (500 U/mL) ± PGE2 (10 nM) ± E7046 (10,100,300,1000,or 3000 nM) for 7 d.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: C57BL/6 mice
  • Dosages: 100 mg/kg or 150 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (206.87 mM)
Ethanol '-1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 483.39
Formula

C22H18F5N3O4

CAS No. 1369489-71-3
Storage powder
in solvent
Synonyms N/A
Smiles CC(C1=CC=C(C=C1)C(=O)O)NC(=O)C2=C(N(N=C2C(F)F)C)OC3=CC=CC(=C3)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02540291 Terminated Drug: E7046 Tumors Eisai Inc. July 30 2015 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID