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Submit ReviewPKI 166 hydrochloride
Description: Potent EGFR-kinase inhibitor
Chemical Name: 4-[4-[[(1R)-1-Phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for PKI 166 hydrochloride
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 for PKI 166 hydrochloride
| M. Wt | 366.84 |
| Formula | C20H18N4O.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2230253-82-2 |
| PubChem ID | 91691117 |
| InChI Key | ZPTWAAIZEGWMGX-BTQNPOSSSA-N |
| Smiles | OC(C=C3)=CC=C3C2=CC1=C(N[C@@H]([C@]4=CC=CC=C4)C)N=CN=C1N2.Cl |
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.
Product Datasheets for PKI 166 hydrochloride
References for PKI 166 hydrochloride
References are publications that support the biological activity of the product.
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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Keywords: PKI 166 hydrochloride, PKI 166 hydrochloride supplier, 187724-61-4, potent, EGFR, kinase, inhibitors, epidermal, growth, factor, receptor, tyrosine, antiangiogenic, antitumor, antitumour, inhibits, PKI166, 4941, Tocris Bioscience
Citations for PKI 166 hydrochloride
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.