2. Apoptosis
  3. Apoptosis
  4. PCC0208017

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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PCC0208017 Chemical Structure

PCC0208017 Chemical Structure

CAS No. : 2623158-64-3

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

PCC0208017 Related Antibodies

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Description

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].

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.

PCC0208017 Related Antibodies

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, 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.

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.
Molecular Weight

403.40

Formula

C19H20F3N7
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (309.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Purity & Documentation
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. 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
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PCC0208017 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PCC02080172623158-64-3PCC 0208017PCC-0208017ApoptosisGliomaMARK3MARK4MoleculardockingInhibitorinhibitorinhibit

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