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Submit ReviewDDR1-IN-1 dihydrochloride
Description: Selective DDR1 inhibitor
Chemical Name: N-[3-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)benzamide dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for DDR1-IN-1 dihydrochloride
DDR1-IN-1 dihydrochloride is a 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 for DDR1-IN-1 dihydrochloride
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 for DDR1-IN-1 dihydrochloride
DDR1-IN-1 dihydrochloride 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 DDR1-IN-1 dihydrochloride
| M. Wt | 625.51 |
| Formula | C30H31F3N4O3.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1780303-76-5 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for DDR1-IN-1 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 62.55 | 100 | |
| DMSO | 31.28 | 50 |
Preparing Stock Solutions for DDR1-IN-1 dihydrochloride
The following data is based on the product molecular weight 625.51. 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 | 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 for DDR1-IN-1 dihydrochloride
References for DDR1-IN-1 dihydrochloride
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for DDR1-IN-1 dihydrochloride, please let us know.
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Keywords: DDR1-IN-1 dihydrochloride, DDR1-IN-1 dihydrochloride supplier, selective, discoidin, domain, receptors, DDR1, DDR2, tyrosine, kinases, Other, RTKs, 5077, Tocris Bioscience
6 Citations for DDR1-IN-1 dihydrochloride
Citations are publications that use Tocris products. Selected citations for DDR1-IN-1 dihydrochloride include:
Piyush B et al (2021) Breast tissue regeneration is driven by cell-matrix interactions coordinating multi-lineage stem cell differentiation through DDR1. Nat Commun 12 7116 PMID: 34893587
Vehlow et al (2019) Interaction of Discoidin Domain Receptor 1 with a 14-3-3-Beclin-1-Akt1 Complex Modulates Glioblastoma Therapy Sensitivity. Cell Rep 26 3672 PMID: 30917320
Mogami (2018) Collagen Type 1 accelerates healing of ruptured fetal membranes. Sci Rep 8 696 PMID: 29330408
Adria et al (2020) Discoidin domain receptor 1-deletion ameliorates fibrosis and promotes adipose tissue beiging, brown fat activity, and increased metabolic rate in a mouse model of cardiometabolic disease. Mol Metab 39 101006 PMID: 32360427
Romayor et al (2020) Silencing of sinusoidal DDR1 reduces murine liver metastasis by colon carcinoma. Sci Rep 10 18398 PMID: 33110221
Malaguarnera et al (2015) Novel cross talk between IGF-IR and DDR1 regulates IGF-IR trafficking, signaling and biological responses. BMC Complement Altern Med 6 16084 PMID: 25840417
Do you know of a great paper that uses DDR1-IN-1 dihydrochloride from Tocris? Please let us know.
Reviews for DDR1-IN-1 dihydrochloride
Average Rating: 5 (Based on 1 Review.)
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Collagen type 1 activated collagen receptor discoidin domain receptor.
By
Anonymous on 02/21/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: 3D Culture Matrix
10 μg/ml treat 24h and 48h
