AMX12006
Based on 1 Customer Validation
AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.9%
- CAS. Nr.: 2639775-01-0
- Formel: C26H22F3N3O3
- Molecular Weight:481.47
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
hEP4 4.3 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
79.47 μM
Compound: 36; AMX12006
|
Cytotoxicity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
|
[PMID: 37312837] |
| CT26.WT | IC50 |
41.39 μM
Compound: 36; AMX12006
|
Cytotoxicity against mouse CT26.WT cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse CT26.WT cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
|
[PMID: 37312837] |
| Lewis lung carcinoma cell line | IC50 |
>100 μM
Compound: 36; AMX12006
|
Cytotoxicity against mouse Lewis lung carcinoma cell line assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse Lewis lung carcinoma cell line assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
|
[PMID: 37312837] |
| MCF7 | IC50 |
46.73 μM
Compound: 36; AMX12006
|
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
|
[PMID: 37312837] |
In Vitro
AMX12006 (compound 36) (0-100 µM) shows cytotoxic with IC50s of 46.73, 79.47, >100, 41.39, >100 µM for MCF-7, 4T1, HCA-7, CT-26 WT, LLC cells, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MCF-7, 4T1, HCA-7, CT-26 WT, LLC cells
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Concentration:0-100 µM
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Incubation Time:
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Result:Showed cytotoxic with IC50s of 46.73, 79.47, >100, 41.39, >100 µM for MCF-7, 4T1, HCA-7, CT-26 WT, LLC cells, respectively.
In Vivo
Pharmacokinetic Parameters of AMX12006 in Sprague-Dawley rats[1].
| iv, 1 mg/kg | po, 10 mg/kg | |
| Tmax (h) | 0.5 | |
| Cmax (ng/mL) | 4627 ± 304 | 8243 ± 370 |
| AUC(0-t)(h·ng/mL) | 3375 ± 477 | 25672 ± 5668 |
| AUC0–∞ (h·ng/mL) | 3416 ± 495 | 25707 ± 5682 |
| T1/2(h) | 1.4 ± 0.3 | 2.7 ± 0.2 |
| CL (mL/min/kg) | 4.95 ± 0.77 | |
| Vdss (L/kg) | 0.41 ± 0.04 | |
| F % | 76.1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2639775-01-0
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Appearance Solid
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Molecular Weight 481.47
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Formel C26H22F3N3O3
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Color White to light yellow
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SMILES
O=C(N[C@@H](C)C1=CC=C(C(O)=O)C=C1)C2=C(C3=CC=CC=C3N2C)NC4=CC(C(F)(F)F)=CC=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMF : 20 mg/mL (41.54 mM; Need ultrasonic and warming)
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)
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
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Data Sheet (276 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
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 |
|---|---|---|---|---|---|
| DMF | 1 mM | 2.0770 mL | 10.3849 mL | 20.7697 mL | 51.9243 mL |
| 5 mM | 0.4154 mL | 2.0770 mL | 4.1539 mL | 10.3849 mL | |
| 10 mM | 0.2077 mL | 1.0385 mL | 2.0770 mL | 5.1924 mL | |
| 15 mM | 0.1385 mL | 0.6923 mL | 1.3846 mL | 3.4616 mL | |
| 20 mM | 0.1038 mL | 0.5192 mL | 1.0385 mL | 2.5962 mL | |
| 25 mM | 0.0831 mL | 0.4154 mL | 0.8308 mL | 2.0770 mL | |
| 30 mM | 0.0692 mL | 0.3462 mL | 0.6923 mL | 1.7308 mL | |
| 40 mM | 0.0519 mL | 0.2596 mL | 0.5192 mL | 1.2981 mL |