JNJ28871063 hydrochloride is an orally active, ATP-competitive, and highly selective pan-ErbB kinase inhibitor with IC50 values of 22 nM for ErbB1, 38 nM for ErbB2, and 21 nM for ErbB4, JNJ28871063 hydrochloride effectively inhibits phosphorylation of key tyrosine residues in EGFR and ErbB2, crossing the blood–brain barrier, and demonstrating antitumor efficacy in xenograft models overexpressing EGFR and ErbB2.

Her1:22 nM, HER2:38 nM

In kinase assays, JNJ28871063 hydrochloride inhibited ErbB1, ErbB2, and ErbB4 with IC50 values of 22-38 nM. In cellular assays, it demonstrated growth inhibition in ErbB-overexpressing cancer cells (IC50 60-168 nM) while showing low potency in low-expression lines (>10 μM). Treatment (3 μM, 16 h) reduced basal ErbB2 phosphorylation in BT474 and SKBR3 cells [1].

In nude mice bearing N87 (gastric cancer) xenografts, oral administration of JNJ28871063 hydrochloride (100 mg/kg/day for 30 days) resulted in a tumor growth inhibition (TGI) of 71%. In an A431 (epidermoid carcinoma) xenograft model, the same dosage produced a TGI of 66.8%. A characteristic of the compound is its ability to cross the blood-brain barrier (BBB), demonstrating activity against intracranial tumors in preclinical models of ErbB-driven cancers [1].

DMSO: 80 mg/mL (154.02 mM), Sonication is recommended.

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (1.93 mM), Sonication is recommended.