Potent EGFR-kinase inhibitor (IC50
= 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable.
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All Tocris products are intended for laboratory research use only.
Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats.
Ulu et al.
Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena.
Kaspersen et al.
Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma.
Bruns et al.
Cancer Res., 2000;60:2926