T025

SKU: orb2901700

Description

T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of4.8, 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.

Key Properties

• CAS Number: 2407433-00-3
• MW: 382.42
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₈N₈
• SMILES: CNc1nc(NCc2ncccn2)c2c(c[nH]c2n1)-c1ccc2ncccc2c1
• Target: CDK
• Solubility: In Vitro: DMSO : 8.25 mg/mL (21.57 mM; Ultrasonic )

Bioactivity

• 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. 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.
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• 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. 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

CDK