2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. JNJ28871063 hydrochloride

JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.

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JNJ28871063 hydrochloride Chemical Structure

JNJ28871063 hydrochloride Chemical Structure

CAS No. : 944342-90-9

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Description

JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2[1].

IC50 & Target[1]

ErbB1

22 nM (IC50)

ErbB2

38 nM (IC50)

ErbB4

21 nM (IC50)

In Vitro

JNJ-28871063 demonstrates potent growth inhibition in vitro of human cancer cell lines (N87; BT474; SKBR3; A431; HN5) overexpressing the ErbB2 receptor with IC50 values with 60-168 nM. 28871063 exhibited the least effect at inhibiting growth of non–ErbB-over-expressing cell lines (HeLa, A375, HCT116, HT29, MRC5 primary fibroblasts cells; IC50>10 μM)[1].
JNJ-28871063 hydrochloride (3 μM; 16 hours) reduces the basal level of ErbB2 phosphorylation in SKBR3 cells[1].
JNJ28871063 hydrochloride is from an aminopyrimidine oxime structural class[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ28871063 hydrochloride Related Antibodies

Western Blot Analysis[1]

Cell Line: BT474 cells
Concentration: 3 μM
Incubation Time: 16 hours
Result: Reduced the basal level of ErbB2 phosphorylation.
In Vivo

JNJ28871063 hydrochloride (100 mg/kg/day; Oral; for 30 days) shows significant inhibition of tumor growth (TGI=71%)[1].
JNJ28871063 hydrochloride produces a significant inhibition of tumor growth at 100 mg/kg (TGI=66.8%) in an A431 human tumor xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice bearing N87 tumor xenografts[1]
Dosage: 100 mg/kg
Administration: Oral; daily for 30 days
Result: Showed significant inhibition of tumor growth (TGI=71%).
Molecular Weight

519.42

Formula

C24H28Cl2N6O3
CAS No.
SMILES

NC1=C(/C=N/OCCN2CCOCC2)C(NC3=CC(Cl)=C(OCC4=CC=CC=C4)C=C3)=NC=N1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JNJ28871063 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ28871063944342-90-9JNJ 28871063JNJ-28871063EGFREpidermal growth factor receptorErbB-1HER1orallyErbBtyrosineresiduesErbB2blood-brainbarrieraminopyrimidineoximeN87BT474SKBR3A431HN5Inhibitorinhibitorinhibit

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