PKI 166 hydrochloride

Pricing Availability   Qty
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)
Literature (1)

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
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.

Solubility Data for PKI 166 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 100
ethanol 50

Preparing Stock Solutions for PKI 166 hydrochloride

The following data is based on the product molecular weight 366.84. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for PKI 166 hydrochloride

Certificate of Analysis / Product Datasheet
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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

If you know of a relevant reference for PKI 166 hydrochloride, please let us know.

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Citations for PKI 166 hydrochloride

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Literature in this Area

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Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.