ASP4132
Based on 1 publication(s) in Google Scholar
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
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- Pureza: 99.81%
- No. CAS: 1640294-30-9
- Fòrmula: C46H51F3N6O8S2
- Peso molecular:937.06
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) ASP4132
MoreVer todos los productos específicos de isoformas AMPK
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Actividad biológica
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AMPK 18 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-435 | EC50 |
0.018 μM
Compound: 28; ASP4132
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Activation of AMPK in human MDA-MB-435 cells measured after 2 hrs by anti-phospho-Acetyl-CoA Carboxylase (Ser79) antibody-based ELISA
Activation of AMPK in human MDA-MB-435 cells measured after 2 hrs by anti-phospho-Acetyl-CoA Carboxylase (Ser79) antibody-based ELISA
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[PMID: 32007387] |
| MDA-MB-453 | IC50 |
0.014 μM
Compound: 28; ASP4132
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Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay
Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay
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[PMID: 32007387] |
| SK-BR-3 | IC50 |
>3 μM
Compound: 28; ASP4132
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Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay
Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay
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[PMID: 32007387] |
ASP4132 shows comparable cell growth inhibitory (IC50=0.014 μM) activity against MDA-MB-453 breast cancer cell[1].
ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC50>3 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ASP4132 (1 mg/kg; IV or PO) has a T1/2 of 3.6 hours, a CLtot of 19 mL/min?kg, and a Vss of 4.6 L/kg for rats for IV[1].
ASP4132 is stable in human liver microsomes (HLM CLint, vitro=61 mL/min?kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five-week-old male nude mice with MDA-MB-453[1]
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Dosage:0.5, 1, 2, 4, 8 mg/kg
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Administration:PO; once daily; for 21 days
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Result:The tumor growth inhibition (TGI) rate was 29% at 1 mg/kg, and the tumor regression rate was 26%, 87% and 96% at 2, 4 and 8 mg/kg, respectively.
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Animal Model:Male SD rats[1]
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Dosage:1 mg/kg (Pharmacokinetic Analysis)
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Administration:IV or PO
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Result:Had a T1/2 of 3.6 hours, a CLtot of 19 mL/min•kg, and a Vss of 4.6 L/kg for rats for IV.
Had a Cmax of 72 ng/mL and an AUC24h of 705 ng∙h/mL for PO.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1640294-30-9
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Appearance Solid
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Peso molecular 937.06
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Fòrmula C46H51F3N6O8S2
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Color White to off-white
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SMILES
O=C(C1=NC2=CC=C(C3CCN(CC4=CC=C(OC)N=C4)CC3)C=C2N1)N5CCN(CC6=CC=C(C(F)(F)F)C=C6)CC5.O=S(C7=CC=C(C)C=C7)(O)=O.O=S(C8=CC=C(C)C=C8)(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
2021 Apr 6;12(4):365. PMID: 33824293
Solvente y solubilidad
DMSO : 100 mg/mL (106.72 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (sealed storage, away from moisture). 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 | 1.0672 mL | 5.3358 mL | 10.6717 mL | 26.6792 mL |
| 5 mM | 0.2134 mL | 1.0672 mL | 2.1343 mL | 5.3358 mL | |
| 10 mM | 0.1067 mL | 0.5336 mL | 1.0672 mL | 2.6679 mL | |
| 15 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7786 mL | |
| 20 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3340 mL | |
| 25 mM | 0.0427 mL | 0.2134 mL | 0.4269 mL | 1.0672 mL | |
| 30 mM | 0.0356 mL | 0.1779 mL | 0.3557 mL | 0.8893 mL | |
| 40 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6670 mL | |
| 50 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5336 mL | |
| 60 mM | 0.0178 mL | 0.0889 mL | 0.1779 mL | 0.4447 mL | |
| 80 mM | 0.0133 mL | 0.0667 mL | 0.1334 mL | 0.3335 mL | |
| 100 mM | 0.0107 mL | 0.0534 mL | 0.1067 mL | 0.2668 mL |
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