Art. -Nr.: HY-139604

PCC0208017

3 Cited Publications

Kundenbewertung

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.52%
CAS. Nr.: 2623158-64-3
Formel: C₁₉H₂₀F₃N₇
Molecular Weight:403.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PCC0208017 Chemical Structure

CAS. Nr.: 2623158-64-3

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

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.

Cell Proliferation Assay^[1]

Cell Line:

The glioma cell lines GL261, U87-MG, U251
Concentration:

0, 3, 6, 9, 12, 15, 18, 21 μM
Incubation Time:

24 hours
Result:

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 Line:
Concentration:

Glioma cell lines GL261 and U251 1, 2, 5 μM
Incubation Time:

24 hours
Result:

Decreased the phosphorylation of Tau.

In Vivo

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, C_max is 1.36 μg/mL and T_max is 0.833 h. In brain, C_max is 0.14 μg/mL and T_max is 0.833 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 mice bearing murine glioma GL261 xenograft tumor^[1]
Dosage:

50 mg/kg and 100 mg/kg (suspended in a 0.5% methylcellulose solution)^[1].
Administration:

Orally administrated every day at a volume of 10 mL/kg
Result:

Inhibited GL261 cells growth in xenograft mouse model.

Chemical Information

CAS. Nr. 2623158-64-3
Appearance Solid
Molecular Weight 403.40
Formel C₁₉H₂₀F₃N₇
Color Off-white to light yellow
SMILES

FC(F)(C1=CN=C(NC2=CC=C3C(CCN(C3)C)=C2)N=C1NCC4=NNC=C4)F
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

All

Sort by:

Journal Impact Factor

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (12.39 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PCC0208017

3 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

PCC0208017

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PCC0208017

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PCC0208017

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PCC0208017

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PCC0208017 Related Classifications

HY-139604 Related Classifications