PCC0208017,2623158-64-3

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PCC0208017

CAS No. : 2623158-64-3

MCE 国际站：PCC0208017

产品活性：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。

研究领域：Apoptosis

作用靶点：Apoptosis

In Vitro: 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.

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).
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.

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