1. Cell Cycle/DNA Damage Apoptosis Protein Tyrosine Kinase/RTK
  2. CDK Apoptosis DYRK
  3. T025

T025 是口服有效的Cdc2-like 激酶 (CLK) 抑制剂,对 CLK1,CLK2,CLK3,CLK4,DYRK1A,DYRK1B 和 DYRK2Kd 分别为4.8,0.096,6.5,0.61,0.074,1.5 和 32 nM。T025 诱导 caspase-3/7 介导的细胞凋亡 (apoptosis)。T025 可降低 CLK 依赖性磷酸化。T025 在血液和实体癌细胞系中均具有抗增殖活性 (IC50值:30-300 nM)。T025 具有抗肿瘤功效,主要用于MYC驱动的疾病研究。

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T025 Chemical Structure

T025 Chemical Structure

CAS No. : 2407433-00-3

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4950
In-stock
1 mg ¥1800
In-stock
5 mg ¥4500
In-stock
10 mg ¥8000
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research[1].

IC50 & Target

CLK2

0.096 nM (Kd)

CLK4

0.61 nM (Kd)

CLK1

4.8 nM (Kd)

CLK3

6.5 nM (Kd)

DYRK1A

0.074 nM (Kd)

DYRK1B

1.5 nM (Kd)

DYRK2

32 nM (Kd)

体外研究
(In Vitro)

T025 (0-1000 nM; 72 hours) significantly suppresses the growth of MDA-MB-468 cells in a dose-dependent manner[1].
T025 (0-1000 nM; 6 hours) reduces phosphorylation levels in MDA-MB-468 cells[1].

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

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 72 hours
Result: Resulted in concentration dependent growth inhibition.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 10, 30, 100, 300 and 1000 nM
Incubation Time: 6 hours
Result: Decreased both pCLK2 and CLK2.
体内研究
(In Vivo)

T025 (50 mg/kg; p.o.; 2, 4, 8 hours, Balb/c nude mice (7 to 8 week-old females).) suppress the CLK-dependent phosphorylation and induce skipping exon in various genes[1].
T025 (50 mg/kg; p.o.; twice daily on 2 days per week, for 3 weeks, Balb/c nude mice (7 to 8 week-old females).) inhibits MDA-MB-468 xenograft mice tumor growth and without affect body weight [1].

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

Animal Model: Balb/c nude mice (7 to 8 week-old females)[1]
Dosage: 50 mg/kg
Administration: Oral administration; 2, 4, 8 hours.
Result: pCLK2 detected with immunohistochemistry and immunoblotting decreased, by a reduction in the RPS6KB1 exon 7 and BCLAF1 exon 11 percentage splice-in (PSI) values.
Animal Model: Balb/c nude mice (7 to 8 week-old females)[1]
Dosage: 50 mg/kg
Administration: Oral administration; twice daily on 2 days per week, for 3 weeks.
Result: Suppressed tumor growth and < 10% nadir body weight loss.
分子量

382.42

Formula

C21H18N8

CAS 号
性状

固体

颜色

Yellow to green

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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 8.25 mg/mL (21.57 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 2.6149 mL 13.0746 mL 26.1493 mL
5 mM 0.5230 mL 2.6149 mL 5.2299 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: 0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (26.15 mM); 悬浊液; Need ultrasonic and warming and heat to 40°C

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

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

纯度: 98.84%

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6149 mL 13.0746 mL 26.1493 mL 65.3731 mL
5 mM 0.5230 mL 2.6149 mL 5.2299 mL 13.0746 mL
10 mM 0.2615 mL 1.3075 mL 2.6149 mL 6.5373 mL
15 mM 0.1743 mL 0.8716 mL 1.7433 mL 4.3582 mL
20 mM 0.1307 mL 0.6537 mL 1.3075 mL 3.2687 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.

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产品名称:
T025
目录号:
HY-112296
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