T025
Based on 4 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.64%
- CAS. Nr.: 2407433-00-3
- Formel: C21H18N8
- Molecular Weight:382.42
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) T025
More
Biologische Aktivität
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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) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468 cells
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Concentration:1, 10, 100 and 1000 nM
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Incubation Time:72 hours
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Result:Resulted in concentration dependent growth inhibition.
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Cell Line:MDA-MB-468 cells
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Concentration:0, 10, 30, 100, 300 and 1000 nM
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Incubation Time:6 hours
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Result:Decreased both pCLK2 and CLK2.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude mice (7 to 8 week-old females)[1]
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Dosage:50 mg/kg
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Administration:Oral administration; 2, 4, 8 hours.
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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.
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Animal Model:Balb/c nude mice (7 to 8 week-old females)[1]
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Dosage:50 mg/kg
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Administration:Oral administration; twice daily on 2 days per week, for 3 weeks.
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Result:Suppressed tumor growth and < 10% nadir body weight loss.
Chemical Information
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CAS. Nr. 2407433-00-3
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Appearance Solid
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Molecular Weight 382.42
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Formel C21H18N8
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Color Yellow to green
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SMILES
CNC1=NC(NCC2=NC=CC=N2)=C(C(C3=CC=C(N=CC=C4)C4=C3)=CN5)C5=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Mol Life Sci
Opposing USP19 splice variants in TGF-β signaling and TGF-β-induced epithelial-mesenchymal transition of breast cancer cells. [Abstract]2023 Jan 17;80(2):43. PMID: 36646950 -
Breast Cancer Res
Pharmacological CLK inhibition disrupts SR protein function and RNA splicing blocking cell growth and migration in TNBC. [Abstract]2025 Jul 29;27(1):140. PMID: 40731028 -
Int J Mol Sci
2023 Apr 4;24(7):6733. PMID: 37047705 -
Lösungsmittel & Löslichkeit
DMSO : 8.25 mg/mL (21.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (26.15 mM); Suspended solution; Need ultrasonic and warming and heat to 40°C
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- Español - ES (393 KB)
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- Italian - IT (393 KB)
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- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6149 mL | 13.0746 mL | 26.1493 mL | 65.3731 mL |
| 5 mM | 0.5230 mL | 2.6149 mL | 5.2299 mL | 13.0746 mL | |
| 10 mM | 0.2615 mL | 1.3075 mL | 2.6149 mL | 6.5373 mL | |
| 15 mM | 0.1743 mL | 0.8716 mL | 1.7433 mL | 4.3582 mL | |
| 20 mM | 0.1307 mL | 0.6537 mL | 1.3075 mL | 3.2687 mL |
T025 Related Classifications
HY-112296 Related Classifications
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