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PCC0208017 is an inhibitor of MARK3 and MARK4 with IC50s of 1.8 and 2.01 nM. PCC0208017 disrupts microtubule dynamics and displays potent antitumor activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $97 | In Stock | |
5 mg | $239 | In Stock | |
10 mg | $383 | In Stock | |
25 mg | $712 | In Stock | |
50 mg | $1,080 | In Stock | |
1 mL x 10 mM (in DMSO) | $263 | In Stock |
Description | PCC0208017 is an inhibitor of MARK3 and MARK4 with IC50s of 1.8 and 2.01 nM. PCC0208017 disrupts microtubule dynamics and displays potent antitumor activity. |
In vitro | PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 (1-5 μM) decreases the phosphorylation of Tau. PCC0208017 (3-21 μM) suppresses the proliferation of glioma cells[1]. |
In vivo | In C57BL/6 mice bearing murine glioma GL261 xenograft tumor, PCC0208017 (50 and 100 mg/kg; oral) dose-dependently inhibits the growth of xenograft tumors derived with inhibition rates of 56.15% and 70.32%, respectively. PCC0208017 (50 mg/kg; oral) exhibits Cmax and Tmax of 1.36 μg/mL and 0.833 h in plasma and 0.14 μg/mL and 0.833 h in brain[1]. Co-treatment of PCC0208017 (50 mg/kg) significantly enhances the anti-tumor activity of Temozolomide (100 mg/kg) with inhibition rates from 34.15% to 83.5%[1]. |
Molecular Weight | 403.4 |
Formula | C19H20F3N7 |
Cas No. | 2623158-64-3 |
Smiles | CN1CCc2cc(Nc3ncc(c(NCc4cc[nH]n4)n3)C(F)(F)F)ccc2C1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 112.5 mg/mL (278.9 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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