PCC0208017

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PCC0208017 

PCC0208017 是有效的微管亲和力调节激酶 MARK3/MARK4 抑制剂，IC50 值分别为 1.8 和 2.01 nM。 PCC0208017 对 MARK1 和 MARK2 的抑制活性要低得多，IC50 值分别为 31.4 和 33.7 nM。 PCC0208017 在体内外都抑制神经胶质瘤进展。PCC0208017 破坏微管动力学并诱导 G2/M 期细胞周期停滞和细胞凋亡。PCC0208017 具有强大的抗肿瘤活性并显示出良好的 BBB 通透性。

PCC0208017

PCC0208017 Chemical Structure

CAS No. : 2623158-64-3

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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[1].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

403.40

Formula

C19H20F3N7
CAS 号

2623158-64-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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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