AAT-008
Based on 1 Customer Validation
AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively. AAT-008 exerts tumor growth delay in mice bearing CT26WT colon tumors when combined with radiotherapy. AAT-008 can be used for the study of acute and chronic inflammatory pain and cancer .
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.03%
- CAS. Nr.: 847727-81-5
- Formel: C21H16ClFN2O4
- Molecular Weight:414.81
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Biologische Aktivität
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EP4 0.97 nM (Ki) |
EP4 6.1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
16.3 nM
Compound: 4j; AAT-008
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Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
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[PMID: 28169162] |
| HEK293 | IC50 |
2.4 nM
Compound: 4j; AAT-008
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Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
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[PMID: 28169162] |
| Species | Dose | Route | T1/2 | AUC0-inf | CLtotal | Vdss | F | Cmax | Tmax |
|---|---|---|---|---|---|---|---|---|---|
| Dog[1] | 1 mg/kg | i.v. | 8.43 h | 7490 ng·h/mL | 2.30 mL/min/kg | 1.21 L/kg | / | / | / |
| Dog[1] | 1 mg/kg | p.o. | 7.95 h | 6080 ng·h/mL | / | / | 80.6 % | 1450 ng/mL | 0.438 h |
| Monkey[1] | 1 mg/kg | i.v. | 14.5 h | 3390 ng·h/mL | 5.31 mL/min/kg | 4.70 L/kg | / | / | / |
| Monkey[1] | 1 mg/kg | p.o. | 21.9 h | 2460 ng·h/mL | / | / | 73.3 % | 76.0 ng/mL | 8 h |
| Rat[1] | 1 mg/kg | i.v. | 4.59 h | 9620 ng·h/mL | 1.75 mL/min/kg | 0.593 L/kg | / | / | / |
| Rat[1] | 1 mg/kg | p.o. | 3.71 h | 7090 ng·h/mL | / | / | 73.6 % | 994 ng/mL | 0.750 h |
AAT-008 (3-30 mg/kg, p.o., once or twice daily, up to 18 days) exerts tumor growth delay in Balb/c mice bearing CT26WT colon tumors alone or combined with radiotherapy[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CT26WT cells (5 × 105) were subcutaneously injected into the right hind legs of 7-week-old female Balb/c mice[2]
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Dosage:3, 10, 30 mg/kg
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Administration:p.o., once or twice daily, up to 18 days
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Result:Showed minimal tumor growth delay alone.
Prolonged tumor doubling time when combined with radiotherapy (9 Gy on day 3).
Increased the mean proportion of intratumoral Teff (CD45+CD8+CD69+).
Chemical Information
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CAS. Nr. 847727-81-5
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Appearance Solid
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Molecular Weight 414.81
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Formel C21H16ClFN2O4
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Color White to off-white
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SMILES
O=C(O)C1=CC=C([C@@H](NC(C2=CC(Cl)=CN=C2OC3=CC=CC(F)=C3)=O)C)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (241.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Okumura Y, et al. Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Bioorg Med Chem Lett. 2017;27(5):1186-1192. [Content Brief]
[2]. Manabe Y, et al. Biological effects of prostaglandin E2-EP4 antagonist (AAT-008) in murine colon cancer in vivo: enhancement of immune response to radiotherapy and potential as a radiosensitizer. Transl Cancer Res. 2023 Feb 28;12(2):351-358. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4107 mL | 12.0537 mL | 24.1074 mL | 60.2686 mL |
| 5 mM | 0.4821 mL | 2.4107 mL | 4.8215 mL | 12.0537 mL | |
| 10 mM | 0.2411 mL | 1.2054 mL | 2.4107 mL | 6.0269 mL | |
| 15 mM | 0.1607 mL | 0.8036 mL | 1.6072 mL | 4.0179 mL | |
| 20 mM | 0.1205 mL | 0.6027 mL | 1.2054 mL | 3.0134 mL | |
| 25 mM | 0.0964 mL | 0.4821 mL | 0.9643 mL | 2.4107 mL | |
| 30 mM | 0.0804 mL | 0.4018 mL | 0.8036 mL | 2.0090 mL | |
| 40 mM | 0.0603 mL | 0.3013 mL | 0.6027 mL | 1.5067 mL | |
| 50 mM | 0.0482 mL | 0.2411 mL | 0.4821 mL | 1.2054 mL | |
| 60 mM | 0.0402 mL | 0.2009 mL | 0.4018 mL | 1.0045 mL | |
| 80 mM | 0.0301 mL | 0.1507 mL | 0.3013 mL | 0.7534 mL | |
| 100 mM | 0.0241 mL | 0.1205 mL | 0.2411 mL | 0.6027 mL |
AAT-008 Related Classifications
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