JNJ 28871063 hydrochloride

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Cat.No. 3352 - JNJ 28871063 hydrochloride | C24H27ClN6O3.HCl | CAS No. 944342-90-9
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
Literature

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.

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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:


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Keywords: Potent ErbB receptor family inhibitors inhibits Epidermal Growth Factors Receptors Her EGFR Receptor Tyrosine Kinases RTKs JNJ28871063 hydrochloride EGFR

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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  • MAPK Signaling
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Schizophrenia Poster

Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.

Pathways for JNJ 28871063 hydrochloride

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