Biological Activity
Potent and selective DYRK1A/B inhibitor (IC50 values are 22 and 68 nM respectively). Selective for DYRK1A/B over a panel of other kinases. Reduces accumulation of quiescent Panc1 pancreatic cancer cells in G0 under serum free conditions. Also induces DNA damage and apoptosis in quiescent Panc1 cells.
Compound Libraries
TC-S 7004 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 498.32 |
| Formula | C23H17Cl2N5O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1386979-55-0 |
| PubChem ID | 57523919 |
| InChI Key | CQKBSRPVZZLCJE-UHFFFAOYSA-N |
| Smiles | O=C(NC3=CC(C(NCC4=CC(Cl)=CC=C4)=O)=CC=C3Cl)C2=CC1=CN=C(OC)N=C1NC2=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.83 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 498.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.01 mL | 10.03 mL | 20.07 mL |
| 5 mM | 0.4 mL | 2.01 mL | 4.01 mL |
| 10 mM | 0.2 mL | 1 mL | 2.01 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Ewton et al (2011) Inactivation of mirk/dyrk1b kinase targets quiescent pancreatic cancer cells. Mol.Cancer Ther. 10 2104 PMID: 21878655
Anderson et al (2013) Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg.Med.Chem.Lett. 15 6610 PMID: 24239188
Keywords: TC-S 7004, supplier, TC-S7004, Mirk, DYRK1B, DYRK1A, potent, inhibitors, inhibits, DYRK, DYRK, Tocris Bioscience
