PKI 166 hydrochloride
Chemical Name: 4-[4-[[(1R)-1-Phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol hydrochloride
Purity: ≥98%
Biological Activity
PKI 166 hydrochloride is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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 -
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.
J.Pharmacol.Exp.Ther., 2013;345:393 -
Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena.
Kaspersen et al.
Bioorg.Chem., 2012;44:35
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