| Size | Price | Stock | Qty |
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| 5mg |
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| ln Vitro |
In addition to lowering Tau phosphorylation, PCC0208017 suppresses MARK3 and MARK4 activity[1]. Tau phosphorylation is reduced upon treatment with PCC0208017 (1–5 μM; 24 hours)[1]. Glioma cells are inhibited from proliferating by PCC0208017 (3–21 μM; 24 hours)[1].
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| ln Vivo |
In vivo, PCC0208017 exhibits strong anticancer activity and good blood-brain barrier permeability. In a dose-dependent manner, PCC0208017 (50 and 100 mg/kg) suppresses the formation of xenograft tumors generated from GL261 cells. The corresponding inhibition rates are 56.15% and 70.32%. Temozolomide (TMZ; 100 mg/kg)'s anti-tumor efficacy is markedly increased when PCC0208017 is co-treated at a dosage of 50 mg/kg. Tumor inhibition rates rise from 34.15% (TMZ alone) to 83.5% (TMZ+PCC0208017)[1]. A single oral dosage of 50 mg/kg was sufficient to detect PCC0208017 in both the brain and plasma after that. Tmax in plasma is 0.833 h, while Cmax is 1.36 μg/mL. The brain has a Tmax of 0.833 hours and a Cmax of 0.14 μg/mL[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: The glioma cell lines GL261, U87-MG, U251 Tested Concentrations: 0, 3, 6, 9, 12, 15, 18, 21 μM Incubation Duration: 24 hrs (hours) Experimental Results: The IC50 values for GL261, U87-MG and U251 were calculated as 2.77, 4.02 and 4.45 μM, respectively. Cell Proliferation Assay[1] Cell Types: Tested Concentrations: Glioma cell lines GL261 and U251 1, 2, 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished the phosphorylation of Tau. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 mice bearing murine glioma GL261 xenograft tumor[1]
Doses: 50 mg/kg and 100 mg/kg (suspended in a 0.5% methylcellulose solution)[1]. Route of Administration: Orally administered every day at a volume of 10 mL/kg Experimental Results: Inhibited GL261 cells growth in xenograft mouse model. |
| References |
[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.
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| Molecular Formula |
C19H20F3N7
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|---|---|
| Molecular Weight |
403.40
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| CAS # |
2623158-64-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
C1(C(NCC2C=CNN=2)=NC(NC2=CC=C3CN(C)CCC3=C2)=NC=1)C(F)(F)F
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 125 mg/mL (309.87 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4789 mL | 12.3946 mL | 24.7893 mL | |
| 5 mM | 0.4958 mL | 2.4789 mL | 4.9579 mL | |
| 10 mM | 0.2479 mL | 1.2395 mL | 2.4789 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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