PCC0208017
Based on 3 publication(s) in Google Scholar
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.
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- Pureza: 99.52%
- No. CAS: 2623158-64-3
- Fòrmula: C19H20F3N7
- Peso molecular:403.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PCC0208017
More
Actividad biológica
PCC0208017 inhibits the activity of MARK3 and MARK4 and decreased the phosphorylation of Tau[1].
PCC0208017 (1-5 μM; 24 hours) treatment results in decreased phosphorylation of Tau, the subtract of MARKs[1].
PCC0208017 (3-21 μM; 24 hours) suppresses the proliferation of glioma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:The glioma cell lines GL261, U87-MG, U251
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Concentration:0, 3, 6, 9, 12, 15, 18, 21 μM
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Incubation Time:24 hours
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Result:The IC50 values for GL261, U87-MG and U251 were calculated as 2.77, 4.02 and 4.45 μM, respectively.
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Cell Line:
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Concentration:Glioma cell lines GL261 and U251 1, 2, 5 μM
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Incubation Time:24 hours
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Result:Decreased the phosphorylation of Tau.
PCC0208017 (after a single oral administration at a dose of 50 mg/kg) could be detected in both plasma and brain following a single oral dose of 50 mg/kg. In plasma, Cmax is 1.36 μg/mL and Tmax is 0.833 h. In brain, Cmax is 0.14 μg/mL and Tmax is 0.833 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice bearing murine glioma GL261 xenograft tumor[1]
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Dosage:50 mg/kg and 100 mg/kg (suspended in a 0.5% methylcellulose solution)[1].
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Administration:Orally administrated every day at a volume of 10 mL/kg
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Result:Inhibited GL261 cells growth in xenograft mouse model.
Chemical Information
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No. CAS 2623158-64-3
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Appearance Solid
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Peso molecular 403.40
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Fòrmula C19H20F3N7
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Color Off-white to light yellow
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SMILES
FC(F)(C1=CN=C(NC2=CC=C3C(CCN(C3)C)=C2)N=C1NCC4=NNC=C4)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Pharmacol Res
Fenofibrate-mediated inhibition of tumor proliferation and progression by modulating the PTPN14/MARK3/Hippo signaling axis. [Abstract]2025 Aug 24:220:107922. PMID: 40858196 -
J Inflamm Res
Rhein Mitigates Lung Injury in Severe Acute Pancreatitis Through the Inhibition of MARK4-Mediated Microtubule Destabilization. [Abstract]2025 Jan 30:18:1395-1412. PMID: 39906137 -
Biochem Biophys Rep
Clinical data investigation identifies MARK3 as an oncogenic driver in castration-resistant prostate cancer. [Abstract]2025 Apr 7:42:102003. PMID: 40248134
Solvente y solubilidad
DMSO : 100 mg/mL (247.89 mM; ultrasonic and warming and heat to 60°C; 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.
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: ≥ 5 mg/mL (12.39 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (12.39 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 (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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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. 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 | 2.4789 mL | 12.3946 mL | 24.7893 mL | 61.9732 mL |
| 5 mM | 0.4958 mL | 2.4789 mL | 4.9579 mL | 12.3946 mL | |
| 10 mM | 0.2479 mL | 1.2395 mL | 2.4789 mL | 6.1973 mL | |
| 15 mM | 0.1653 mL | 0.8263 mL | 1.6526 mL | 4.1315 mL | |
| 20 mM | 0.1239 mL | 0.6197 mL | 1.2395 mL | 3.0987 mL | |
| 25 mM | 0.0992 mL | 0.4958 mL | 0.9916 mL | 2.4789 mL | |
| 30 mM | 0.0826 mL | 0.4132 mL | 0.8263 mL | 2.0658 mL | |
| 40 mM | 0.0620 mL | 0.3099 mL | 0.6197 mL | 1.5493 mL | |
| 50 mM | 0.0496 mL | 0.2479 mL | 0.4958 mL | 1.2395 mL | |
| 60 mM | 0.0413 mL | 0.2066 mL | 0.4132 mL | 1.0329 mL | |
| 80 mM | 0.0310 mL | 0.1549 mL | 0.3099 mL | 0.7747 mL | |
| 100 mM | 0.0248 mL | 0.1239 mL | 0.2479 mL | 0.6197 mL |
PCC0208017 Related Classifications
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