2. Cell Cycle/DNA Damage Apoptosis
  3. MARK Apoptosis
  4. 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。

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PCC0208017 Chemical Structure

PCC0208017 Chemical Structure

CAS No. : 2623158-64-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3190
In-stock
1 mg ￥1160
In-stock
5 mg ￥2900
In-stock
10 mg ￥4500
In-stock
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

PCC0208017 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

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

PCC0208017 相关抗体:

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].

MCE 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
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (309.87 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

PCC0208017 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4789 mL 12.3946 mL 24.7893 mL 61.9732 mL
5 mM 0.4958 mL 2.4789 mL 4.9579 mL 12.3946 mL
10 mM 0.2479 mL 1.2395 mL 2.4789 mL 6.1973 mL
15 mM 0.1653 mL 0.8263 mL 1.6526 mL 4.1315 mL
20 mM 0.1239 mL 0.6197 mL 1.2395 mL 3.0987 mL
25 mM 0.0992 mL 0.4958 mL 0.9916 mL 2.4789 mL
30 mM 0.0826 mL 0.4132 mL 0.8263 mL 2.0658 mL
40 mM 0.0620 mL 0.3099 mL 0.6197 mL 1.5493 mL
50 mM 0.0496 mL 0.2479 mL 0.4958 mL 1.2395 mL
60 mM 0.0413 mL 0.2066 mL 0.4132 mL 1.0329 mL
80 mM 0.0310 mL 0.1549 mL 0.3099 mL 0.7747 mL
100 mM 0.0248 mL 0.1239 mL 0.2479 mL 0.6197 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PCC02080172623158-64-3PCC 0208017PCC-0208017MARKApoptosisMicrotubule affinity regulating kinaseGliomaMARK3MARK4MoleculardockingInhibitorinhibitorinhibit

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