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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $48 | In Stock | In Stock | |
| 10 mg | $68 | In Stock | In Stock | |
| 25 mg | $130 | In Stock | In Stock | |
| 50 mg | $225 | In Stock | In Stock |
| 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 |
| Smiles | C[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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (206.87 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.83 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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