JNJ 28871063 hydrochlorideA potent inhibitor of ErbB receptors

JNJ 28871063 hydrochloride (CAS 944341-54-2)

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Synonym: 5E-4-Amino-6-(4-benzyloxy-3-chlorophenylamino)pyrimidine-5-carboxaldehyde N-(2-morpholin-4-ylethyl) oxime hydrochloride
Application: A potent inhibitor of ErbB receptors
CAS Number: 944341-54-2
Purity: >97%
Molecular Weight: 519.42
Molecular Formula: C24H27CIN6O3•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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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). JNJ 28871063 hydrochloride is an inhibitor of ErbB-4 and Neu.


References

Contessa and Hamstra (2008) Revoking the privilege: targeting HER2 in the central nervous system. Mol.Pharmacol. 73 271. 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. Guessous et al (2008) Signaling pathways in medulloblastoma. J.Cell.Phys. 217 577.

Physical State :
Solid
Solubility :
Soluble in DMSO (50 mM).
Storage :
Store at 4° C
Refractive Index :
n20D ~1.64 (Predicted)
IC50 :
ErbB4: IC50 = 21 nM; EGFR : IC50 = 22 nM; ErbB2 : IC50 = 38 nM; EGF-induced EFGR: IC50 = 107 nM; Basal HER2: IC50 = 223 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
17747413
MDL Number :
MFCD12828762
SMILES :
C1COCCN1CCON=CC2=C(N=CN=C2NC3=CC(=C(C=C3)OCC4=CC=CC=C4)Cl)N.Cl

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Certificate of Analysis

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JNJ 28871063 hydrochloride  Product Citations

See how others have used JNJ 28871063 hydrochloride. Click on the entry to view the PubMed entry .

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PMID: # 27079641  Loos, M. et al. 2016. Eur. J. Pharmacol. 781: 157-63.

Citations 1 to 1 of 1 total
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