产品
编 号:F618309
分子式:C21H18N8
分子量:382.42
产品类型
结构图
CAS No: 2407433-00-3
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产品详情
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.
体内研究:
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 .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.