Biological Activity
Potent c-Src kinase inhibitor (IC50 = 1.3 nM). Also potent inhibitor of discoidin domain receptor 2 (DDR2) family tyrosine kinases, BTK and Syk. Suppresses LPS-induced activation of macrophages and TGF-β1- induced activation of fibroblasts in vitro. Also inhibits activation of macrophages and fibroblasts and suppresses scar formation in a wound healing model.
Technical Data
| M. Wt | 490.45 |
| Formula | C24H23N3O2S.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| PubChem ID | 121513872 |
| InChI Key | OEWGAUGZPPUIPF-UHFFFAOYSA-N |
| Smiles | OC1=CC=CC(NC2=CC=NC3=C2SC(C4=CC=CC(CN5CCOCC5)=C4)=C3)=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 | 49.05 | 100 | |
| water | 49.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 490.45. 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 | 2.04 mL | 10.19 mL | 20.39 mL |
| 5 mM | 0.41 mL | 2.04 mL | 4.08 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.04 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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References
References are publications that support the products' biological activity.
Sun et al (2012) LCB 03-0110, a novel pan-discoidin domain receptor/c-Src family tyrosine kinase inhibitor, suppresses scar formation by inhibiting fibroblast and macrophage activation. J.Pharmacol.Exp.Ther. 340 510 PMID: 22128347
Keywords: LCB 03-0110 dihydrochloride, supplier, src, kinase, inhibitors, inhibits, potent, discoidin, domain, receptor, DDR, wound, healing, Bruton's, tyrosine, BTK, syk, anti-inflammatory, potent, Src, Kinases, Brutons, Tyrosine, Kinase, (BTK), Syk, Kinase, Other, RTKs, Src, Kinases, Tocris Bioscience
