PCC0208017|cas:2623158-64-3|西域试剂

PCC0208017,98.03%

产品编号：Bellancom-139604| CAS NO：2623158-64-3| 分子式：C₁₉H₂₀F₃N₇| 分子量：403.40

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货号	价格	库存与货期
Bellancom-139604	￥3500.00	杭州北京（现货）
Bellancom-139604	￥5800.00	杭州北京（现货）
Bellancom-139604	￥11000.00	杭州北京（现货）

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PCC0208017

产品介绍

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。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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).
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.

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (309.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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
10 mM	0.2479 mL	1.2395 mL	2.4789 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式