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Purity: ≥98%
ONO-AE3-208 is a novel and potent EP4 antagonist with Ki of 1.3 nM. ONO-AE3-208 inhibits prostate cancer cell invasion, migration, and metastasis. ONO-AE3-208 inhibited in vitro cell invasion and migration in a dose-dependent manner while having no effect on cell proliferation. Treatment with ONO-AE3-208 also suppressed PC3's in vivo bone metastasis. The degree of prostate cancer cell invasiveness was found to be correlated with the expression of EP4, and the EP4 specific antagonist ONO-AE3-208 was found to inhibit cell invasion, migration, and bone metastasis. These findings suggest that EP4 expression levels could be a promising new therapeutic approach for treating metastatic prostate cancer.
| Targets |
FP ( Ki = 790 nM ); TP Receptor ( Ki = 2400 nM ); EP4 ( Ki = 1.3 nM ); EP3 ( Ki = 30 nM )
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| ln Vitro |
ONO-AE3-208 inhibits in vitro cell migration and invasion in a dose-dependent way while having no effect on cell proliferation[2]. When the EET synthesis inhibitor MS-PPOH is present, ONO-AE3-208 eliminates CTGF. Arachidonic acid (AA) causes the attached Af-Art to dilate in a dose-dependent manner; ONO-AE3-208 blocks this effect[3].
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| ln Vivo |
ONO-AE3-208 inhibits PC3 cell metastasis to the bone in vivo in mice[2]. When comparing the photon tumor burdens in the ONO-AE3-208-treated group and the control group, there is a significant time-dependent increase in the former. Compared to the latter, the former has a noticeably higher rate of metastasis formation. In the ONO-AE3-208-treated animals, the median time of metastasis formation is 29 days, whereas in the control group, it is 21 days[4].
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| References |
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| Molecular Formula |
C24H21FN2O3
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|---|---|
| Molecular Weight |
404.4335
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| Exact Mass |
404.15
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| Elemental Analysis |
C, 71.27; H, 5.23; F, 4.70; N, 6.93; O, 11.87
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| CAS # |
402473-54-5
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| Appearance |
Solid powder
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| SMILES |
CC(C1=CC=C(C2=CC=CC=C21)F)C(=O)NC3=C(C=CC(=C3)C#N)CCCC(=O)O
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| InChi Key |
MTDIMKNAJUQTIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H21FN2O3/c1-15(18-11-12-21(25)20-7-3-2-6-19(18)20)24(30)27-22-13-16(14-26)9-10-17(22)5-4-8-23(28)29/h2-3,6-7,9-13,15H,4-5,8H2,1H3,(H,27,30)(H,28,29)
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| Chemical Name |
4-[4-cyano-2-[2-(4-fluoronaphthalen-1-yl)propanoylamino]phenyl]butanoic acid
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| Synonyms |
AE 3-208; AE-3-208; AE3-208; ONO AE3 208; ONO-AE3-208; ONO-AE-3-208; ONO-AE 3-208
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~33.33 mg/mL (~82.4 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5%DMSO + 40%PEG300 + 5%Tween 80 + 50%ddH2O: 4.05mg/ml (10.01mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4726 mL | 12.3631 mL | 24.7262 mL | |
| 5 mM | 0.4945 mL | 2.4726 mL | 4.9452 mL | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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