PKI 166 hydrochloride
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.
|Storage||Store at +4°C|
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 100 mM in DMSO and to 50 mM in ethanol|
Preparing Stock Solutions
The following data is based on the product molecular weight 366.84. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.73 mL||13.63 mL||27.26 mL|
|5 mM||0.55 mL||2.73 mL||5.45 mL|
|10 mM||0.27 mL||1.36 mL||2.73 mL|
|50 mM||0.05 mL||0.27 mL||0.55 mL|
References are publications that support the products' biological activity.
Bruns et al (2000) 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. Cancer Res. 60 2926 PMID: 10850439
Ulu et al (2013) Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. J.Pharmacol.Exp.Ther. 345 393 PMID: 23528611
Kaspersen et al (2012) Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena. Bioorg.Chem. 44 35 PMID: 22832269
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