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E7046

🥰Excellent
Catalog No. TQ0025Cas No. 1369489-71-3

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

E7046

E7046

🥰Excellent
Purity: 99.86%
Catalog No. TQ0025Cas No. 1369489-71-3
E7046 is a specific, orally bioavailable EP4 antagonist (IC50: 13.5 nM, Ki: 23.14 nM), exhibiting anti-tumor activities.
Pack SizePriceAvailabilityQuantity
5 mg$48In Stock
10 mg$68In Stock
25 mg$130In Stock
50 mg$225In Stock
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Purity:99.86%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight483.4
FormulaC22H18F5N3O4
Cas No.1369489-71-3
SmilesC[C@H](NC(=O)c1c(nn(C)c1Oc1cccc(c1)C(F)(F)F)C(F)F)c1ccc(cc1)C(O)=O
Relative Density.1.43 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (206.87 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0687 mL10.3434 mL20.6868 mL103.4340 mL
5 mM0.4137 mL2.0687 mL4.1374 mL20.6868 mL
10 mM0.2069 mL1.0343 mL2.0687 mL10.3434 mL
20 mM0.1034 mL0.5172 mL1.0343 mL5.1717 mL
50 mM0.0414 mL0.2069 mL0.4137 mL2.0687 mL
100 mM0.0207 mL0.1034 mL0.2069 mL1.0343 mL

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