Afatinib, also known as BIW-2992, is an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinases. Afatinib suppresses EGF-induced EGFR phosphorylation and cellular proliferation in various cell lines, including EGFR-overexpressing and HER2-expressing cell lines A431, NIH-3T3-HER2, NCI-N87 and BT-474.

BIW-2992

≥95% by HPLC.

Afatinib inhibited the EGFR kinase (IC50 = 15 nM) using BPS Bioscience EGFR assay performed using 10 µM ATP and 0.2 mg/ml poly-(Glu-Tyr). Activity was measured by Kinase-Glo Plus reagents (Promega).

Soluble in DMSO at 200 mg/ml; soluble in ethanol at 25 mg/ml; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.

White crystalline powder.

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

Eskens, F.A., et al. Br. J. Cancer 98: 80-85 (2008).

Kinase

Inhibitor