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Submit ReviewJNJ 28871063 hydrochloride
Description: Potent ErbB receptor family inhibitor
Chemical Name: 5E-4-Amino-6-(4-benzyloxy-3-chlorophenylamino)pyrimidine-5-carboxaldehyde N-(2-morpholin-4-ylethyl) oxime hydrochloride
Purity: ≥97% (HPLC)
Biological Activity for JNJ 28871063 hydrochloride
JNJ 28871063 hydrochloride is a 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.
Compound Libraries for JNJ 28871063 hydrochloride
JNJ 28871063 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JNJ 28871063 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JNJ 28871063 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.97 | 50 |
Preparing Stock Solutions for JNJ 28871063 hydrochloride
The following data is based on the product molecular weight 519.42. 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 |
|---|---|---|---|
| 0.5 mM | 3.85 mL | 19.25 mL | 38.5 mL |
| 2.5 mM | 0.77 mL | 3.85 mL | 7.7 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.85 mL |
| 25 mM | 0.08 mL | 0.39 mL | 0.77 mL |
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Product Datasheets for JNJ 28871063 hydrochloride
References for JNJ 28871063 hydrochloride
References are publications that support the biological activity of the product.
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: 18651559
If you know of a relevant reference for JNJ 28871063 hydrochloride, please let us know.
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Citations for JNJ 28871063 hydrochloride
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
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