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E7046

Catalog No. TQ0025   CAS 1369489-71-3

E7046 is a specific, orally bioavailable EP4 antagonist (IC50: 13.5 nM, Ki: 23.14 nM), exhibiting anti-tumor activities.

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E7046 Chemical Structure
E7046, CAS 1369489-71-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 48.00
10 mg In stock $ 68.00
25 mg In stock $ 130.00
50 mg In stock $ 225.00
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Purity: 99.09%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description E7046 is a specific, orally bioavailable EP4 antagonist (IC50: 13.5 nM, Ki: 23.14 nM), exhibiting anti-tumor activities.
Targets&IC50 EP4:13.5 nM, EP4:23.14 nM (Ki)
In vitro Through selective EP4 antagonism, E7046 reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells [1].
In vivo E7046 (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. The blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells [1]. In the CT-26 tumor model, the E7046/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of E7046 and RT also produces significantly better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors [2].
Molecular Weight 483.4
Formula C22H18F5N3O4
CAS No. 1369489-71-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (206.87 mM)

TargetMolReferences and Literature

1. Diana I. Albu, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. OncoImmunology. 2. X. Bao, et al. Combination of a Novel EP4 Antagonist E7046 and Radiation Therapy Promotes Anti-tumor Immune Response and Tumor Rejection in Preclinical Tumor Models. International Journal of Radiation Oncology Biology Physics

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library GPCR Compound Library Bioactive Compound Library Clinical Compound Library NO PAINS Compound Library Endocrinology-Hormone Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library

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Keywords

E7046 1369489-71-3 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor Inhibitor E 7046 inhibit E-7046 inhibitor

 

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