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Description: Potent and selective DYRK1A/B inhibitor
Chemical Name: N-[2-Chloro-5-[[[(3-chlorophenyl)methyl]amino]carbonyl]phenyl]-7,8-dihydro-2-methoxy-7-oxopyrido[2,3-d]pyrimidine-6-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for TC-S 7004
TC-S 7004 is a 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 for TC-S 7004
TC-S 7004 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for TC-S 7004
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TC-S 7004
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.83 | 100 |
Preparing Stock Solutions for TC-S 7004
The following data is based on the product molecular weight 498.32. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for TC-S 7004
References for TC-S 7004
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for TC-S 7004, please let us know.
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Keywords: TC-S 7004, TC-S 7004 supplier, TC-S7004, Mirk, DYRK1B, DYRK1A, potent, inhibitors, inhibits, DYRK, 5088, Tocris Bioscience
1 Citation for TC-S 7004
Citations are publications that use Tocris products. Selected citations for TC-S 7004 include:
Blake et al (2019) Application of a MYC degradation screen identifies sensitivity to CDK9 inhibitors in KRAS-mutant pancreatic cancer. Sci Signal 12 PMID: 31311847
Do you know of a great paper that uses TC-S 7004 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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