PKI 166 hydrochloride: R&D Systems
Catalog Number: 4941
Chemical Name: 4-[4-[[(1R)-1-Phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol hydrochloride
Biological Activity
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
  • M.Wt:
    366.84
  • Formula:
    C20H18N4O.HCl
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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
  2. Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena.
    Kaspersen et al.
    Bioorg.Chem., 2012;44:35
  3. 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

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