Biological Activity
Selective discoidin domain receptor 1 (DDR1) tyrosine kinase inhibitor (IC50 values are 105 and 413 nM for DDR1 and DDR2 respectively). Inhibits integrin-induced DDR1 autophosphorylation in an osteosarcoma cell line.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of DDR1-IN-1 is reviewed on the chemical probes website.
Compound Libraries
DDR1-IN-1 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 625.51 |
| Formula | C30H31F3N4O3.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| PubChem ID | 90489006 |
| InChI Key | PBUOJKYQZINPKD-UHFFFAOYSA-N |
| Smiles | CC1=C(OC4=CC(CC(N5)=O)=C5C=C4)C=C(NC(C2=CC=C(CN3CCN(CC)CC3)C(C(F)(F)F)=C2)=O)C=C1.Cl.Cl |
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 | 31.28 | 50 | |
| water | 62.55 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 625.51. 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 | 1.6 mL | 7.99 mL | 15.99 mL |
| 5 mM | 0.32 mL | 1.6 mL | 3.2 mL |
| 10 mM | 0.16 mL | 0.8 mL | 1.6 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kim et al (2013) Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS.Chem.Biol. 8 2145 PMID: 23899692
Canning et al (2014) Structural Mechanisms Determining Inhibition of the Collagen Receptor DDR1 by Selective and Multi-Targeted Type II Kinase Inhibitors. J.Mol.Biol. 426 2457 PMID: 24768818
Keywords: DDR1-IN-1 dihydrochloride, supplier, selective, discoidin, domain, receptors, DDR1, DDR2, tyrosine, kinases, Other, RTKs, Other, RTKs, Tocris Bioscience
