PCC0208017 |
Catalog No.GC65253
One-Click Copy Product Info
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PCC0208017 is a potent microtubule affinity regulating kinase MARK3/MARK4 inhibitor with IC50 values of 1.8 and 2.01 nM, respectively. PCC0208017 exhibits significantly lower inhibitory activity against MARK1 and MARK2, with IC50 values of 31.4 and 33.7 nM, respectively. PCC0208017 inhibits glioma progression both in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and apoptosis. PCC0208017 possesses potent antitumor activity and demonstrates good blood-brain barrier permeability.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2623158-64-3
Sample solution is provided at 25 µL, 10mM.
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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[1].
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].
PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability. PCC0208017 (50 and 100 mg/kg; orally administrated) inhibits the growth of xenograft tumors derived from GL261 cells in a dose-dependent manner. Inhibition rates are 56.15% and 70.32%, respectively. Co-treatment of PCC0208017 at dosage of 50 mg/kg significantly enhances the anti-tumor activity of Temozolomide (TMZ; 100 mg/kg), with an increase in tumor inhibition rates from 34.15% (TMZ only) to 83.5% (TMZ+PCC0208017)[1].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].
[1]. Fangfang Li, et al. PCC0208017, a novel small-molecule inhibitor of MARK3/MARK4, suppresses glioma progression in vitro and in vivo. Acta Pharm Sin B.2020 Feb;10(2):289-300.
| Cas No. | 2623158-64-3 | SDF | |
| Formula | C19H20F3N7 | M.Wt | 403.4 |
| Solubility | DMSO : 125 mg/mL (309.87 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4789 mL | 12.3946 mL | 24.7893 mL |
| 5 mM | 495.8 μL | 2.4789 mL | 4.9579 mL |
| 10 mM | 247.9 μL | 1.2395 mL | 2.4789 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)