PPA24
Based on 1 Customer Validation
PPA24 is a PP2A activator with a KD of 8.465 μM for PP2ACα. PPA24 induces cancer cell death via apoptosis. PP2ACα induces ROS generation and decreases the level of c-Myc expression. PPA24 can be used to study colorectal cancer (CRC), Folinic acid (HY-17556), 5-Fluorouracil (HY-90006), and Oxaliplatin (HY-17371) (FOLFOX)-resistant CRC, and melanoma cancer.
For research use only. We do not sell to patients.
- Purity: 98.09%
- CAS No.: 3035032-77-7
- Formula: C22H27BrClN5S
- Molecular Weight:508.91
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
|
PP2A |
GSK-3α |
GSK-3β |
PPA24 (0.5-50 μM, 48 h) shows cytotoxicity against HCT116, HT29, DLD1, SW480, FOLFOX HCT116 and FOLFOX HT29, with IC50s of 3.95, 6.75, 3.45, 3.64, 2.63 and 3.04 μM, respectively, shows weak cytotoxicity against HaCaT, with IC50 of 10.04 μM[1].
PPA24 (2.5-10 μM, 24 h) induces apoptosis in HCT116, HT29, FOLFOX HCT116, FOLFOX HT29 cells[1].
PPA24 (2.5-5 μM, 6-12 h) stimulates ROS generation in HCT116 cells[1].
PPA24 (2.5-5 μM, 24 h) decreases the level of c-Myc expression in HCT116, FOLFOX HCT116 cells[1].
PPA24 (0.1-10 μM, 48 h) shows a synergistic effect and Gemcitabine (HY-17026) or Cisplatin (HY-17394) with HCT116 cells[1].
PPA24 shows cytotoxicity against SK-MEL-2, SK-MEL-28, A375, Mel1241, and 451Lu cells with IC50s in the range of 5.99-14.45 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, HT29, FOLFOX HCT116, FOLFOX HT29
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Induced apoptosis.
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Cell Line:HCT116, FOLFOX HCT116
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Concentration:2.5 μM, 5 μM
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Incubation Time:24 h
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Result:Decreased the level of c-Myc expression, did not increase the level of degradation of c-Myc.
Reduced the protein expression level of GSK-3α/β but did not change p-GSK-3α/β (S21/9).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 (1.5 × 106) xenografts nude mice model[1]
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Dosage:6 mg/kg, nanoformulation (Nano-PPA24)
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Administration:i.v., three times per week, 23 days
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Result:Inhibited tumor growth with no significant changes in body weight.
Chemical Information
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CAS No. 3035032-77-7
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Appearance Solid
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Molecular Weight 508.91
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Formula C22H27BrClN5S
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Color White to off-white
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SMILES
ClC1=CC=C2C(N(C3=CC=CC=C3S2)CCCC[N+]4(C[N@@](C5)C6)C[N@@]6C[N@@]5C4)=C1.[Br-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (196.50 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 (4.91 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 (4.91 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.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 1.9650 mL | 9.8249 mL | 19.6498 mL | 49.1246 mL |
| 5 mM | 0.3930 mL | 1.9650 mL | 3.9300 mL | 9.8249 mL | |
| 10 mM | 0.1965 mL | 0.9825 mL | 1.9650 mL | 4.9125 mL | |
| 15 mM | 0.1310 mL | 0.6550 mL | 1.3100 mL | 3.2750 mL | |
| 20 mM | 0.0982 mL | 0.4912 mL | 0.9825 mL | 2.4562 mL | |
| 25 mM | 0.0786 mL | 0.3930 mL | 0.7860 mL | 1.9650 mL | |
| 30 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6375 mL | |
| 40 mM | 0.0491 mL | 0.2456 mL | 0.4912 mL | 1.2281 mL | |
| 50 mM | 0.0393 mL | 0.1965 mL | 0.3930 mL | 0.9825 mL | |
| 60 mM | 0.0327 mL | 0.1637 mL | 0.3275 mL | 0.8187 mL | |
| 80 mM | 0.0246 mL | 0.1228 mL | 0.2456 mL | 0.6141 mL | |
| 100 mM | 0.0196 mL | 0.0982 mL | 0.1965 mL | 0.4912 mL |