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JNJ 28871063 hydrochloride

Cat. No. 3352

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Chemical Name: 5E-4-Amino-6-(4-benzyloxy-3-chlorophenylamino)pyrimidine-5-carboxaldehyde N-(2-morpholin-4-ylethyl) oxime hydrochloride

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:

C₂₄H₂₇CIN₆O₃.HCl

Solubility:

Soluble to 50 mM in DMSO

Purity:

>97 %

Storage:

Desiccate at +4°C

CAS No:

944341-54-2

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

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.

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