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T025
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
T025图片
CAS NO:2407433-00-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
T025 是口服有效的Cdc2-like 激酶 (CLK)抑制剂,对 CLK1,CLK2,CLK3,CLK4,DYRK1A,DYRK1B 和 DYRK2 的Kd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。
生物活性

T025 is an orally active and highly potent inhibitor ofCdc2-like kinase (CLKs), withKdvalues of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B andDYRK2, respectively. T025 induces caspase-3/7-mediated cellapoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solidcancercell lines (IC50values: 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].

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].

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

性状

Solid

Formula

C21H18N8

CAS 号

2407433-00-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 8.25 mg/mL(21.57 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6149 mL13.0746 mL26.1493 mL
5 mM0.5230 mL2.6149 mL5.2299 mL
10 mM0.2615 mL1.3075 mL2.6149 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。