产品
编 号：F741684
分子式：C19H20F3N7
分子量：403.4
分子式：C19H20F3N7
分子量：403.4
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 2623158-64-3
产品详情
生物活性：
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.
体内研究：
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).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.Animal Model:C57BL/6 mice bearing murine glioma GL261?xenograft tumor
Dosage:50?mg/kg and 100?mg/kg (suspended in a 0.5% methylcellulose solution).
Administration:Orally administrated every day at a volume of 10?mL/kg
Result:Inhibited GL261?cells growth in xenograft mouse model.
体外研究：
PCC0208017 inhibits the activity of MARK3 and MARK4 and decreased the phosphorylation of Tau.PCC0208017 (1-5 μM; 24?hours) treatment results in decreased phosphorylation of Tau, the subtract of MARKs.PCC0208017 (3-21 μM; 24?hours) suppresses the proliferation of glioma cells.
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.
体内研究：
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).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.Animal Model:C57BL/6 mice bearing murine glioma GL261?xenograft tumor
Dosage:50?mg/kg and 100?mg/kg (suspended in a 0.5% methylcellulose solution).
Administration:Orally administrated every day at a volume of 10?mL/kg
Result:Inhibited GL261?cells growth in xenograft mouse model.
体外研究：
PCC0208017 inhibits the activity of MARK3 and MARK4 and decreased the phosphorylation of Tau.PCC0208017 (1-5 μM; 24?hours) treatment results in decreased phosphorylation of Tau, the subtract of MARKs.PCC0208017 (3-21 μM; 24?hours) suppresses the proliferation of glioma cells.
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