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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 ( IC 50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell Line: MDA-MB-468 cells Concentration: 0, 10, 30, 100, 300 and 1000 nM Incubation Time: 6 hours Result: Decreased both pCLK2 and CLK2. 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 . 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) 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 Form:Solid 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)
中文名称
T025
英文名称
T025
中文别名
-
英文别名
-
CAS号
2407433-00-3
分子式
C21H18N8
分子量
382.42 g/mol
精确质量
≥98%
PSA
104.000 Ų
Logp
3
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T025 97% 5mg

源叶 T025 97% 5mg,2407433-00-3,规格齐全,生产科研实验检测,科学材料数智化一站式易购平台。

品牌:源叶
货号:S23807-5mg
级别: -
货期:30天
已售 519 件
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