Biological Activity
Potent and selective ErbB receptor family inhibitor (IC50 values are 21, 22 and 38 nM for ErbB4, EGFR and ErbB2 respectively). Displays potent growth inhibition of human cancer cell lines overexpressing ErbB2 in vitro (IC50 = 60 - 168 nM) and inhibits growth of human tumor xenografts in vivo. Brain penetrant and orally active.
Technical Data
| M. Wt | 519.42 |
| Formula | C24H27ClN6O3.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 944342-90-9 |
| PubChem ID | 17747413 |
| InChI Key | ZXKZRKQMKNRZNN-GZPZNDDGSA-N |
| Smiles | NC1=C(/C=N/OCCN2CCOCC2)C(NC3=CC(Cl)=C(OCC4=CC=CC=C4)C=C3)=NC=N1.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 | 25.97 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 519.42. 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 | 1.93 mL | 9.63 mL | 19.25 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.85 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Contessa and Hamstra (2008) Revoking the privilege: targeting HER2 in the central nervous system. Mol.Pharmacol. 73 271 PMID: 17981994
Emanuel et al (2008) Cellular and in vivo activity of JNJ-28871063, a nonquinazoline pan-ErbB kinase inhibitor that crosses the blood-brain barrier and displays efficacy against intracranial tumors. Mol.Pharmacol. 73 338 PMID: 17975007
Guessous et al (2008) Signaling pathways in medulloblastoma. J.Cell.Phys. 217 577 PMID:
Keywords: JNJ 28871063 hydrochloride, supplier, Potent, ErbB, receptor, family, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, Her, EGFR, Receptor, Tyrosine, Kinases, RTKs, JNJ28871063, hydrochloride, EGFR, EGFR, Tocris Bioscience
