JNJ 28871063 hydrochloride

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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)
Datasheet
Citations
Reviews
Literature (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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


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Citations for JNJ 28871063 hydrochloride

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Literature in this Area

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Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.