T025|cas:2407433-00-3|西域试剂

T025,98.84%

产品编号：Bellancom-112296| CAS NO：2407433-00-3| 分子式：C₂₁H₁₈N₈| 分子量：382.42

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货号	价格	库存与货期
Bellancom-112296	￥4500.00	杭州北京（现货）
Bellancom-112296	￥8000.00	杭州北京（现货）
Bellancom-112296	￥16500.00	杭州北京（现货）

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T025

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 K_d 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 of Cdc2-like kinase (CLKs), with K_d 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.

体外研究

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

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

Cell Viability Assay

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

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.
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 .

西域 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)
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)
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.

体内研究

西域 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)
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)
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.

体内研究

西域 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)
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)
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.

性状

Solid

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 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
10 mM	0.2615 mL	1.3075 mL	2.6149 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°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