| Chemical Properties | Back Directory | [density ]
1.432±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 8.25 mg/mL (21.57 mM; Need ultrasonic) | [form ]
Solid | [pka]
13.45±0.50(Predicted) | [color ]
Yellow to green |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Biological Activity]
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[1].
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].
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]. | [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.
|
| [IC 50]
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) | [storage]
Store at -20°C | [References]
[1]. Iwai K, et al. Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability. EMBO Mol Med. 2018 Jun;10(6):e8289. |
|
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
|