[CAS NO. 2407433-00-3] T025
PRODUCTS SPECIFICATIONS [2407433-00-3]
DESCRIPTION [2407433-00-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 382.42 |
| Molecular Formula | C21H18N8 |
| SMILES | CNC1=NC(NCC2=NC=CC=N2)=C(C(C3=CC=C(N=CC=C4)C4=C3)=CN5)C5=N1 |
1 Publications Citing Use of MCE
Summary
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 [1] .
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) |
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| 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 [1]
| 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. |
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]
.
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) [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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 8.25 mg/mL ( 21.57 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |