PKI 166 hydrochloride

Name: PKI 166 hydrochloride
Brand: Tocris Bioscience
SKU: 4941

Tocris Bioscience, part of Bio-Techne | Catalog # 4941

COA / SDS

Potent EGFR-kinase inhibitor

Key Product Details

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)
Molecular Weight:	366.84

View Full Technical Details for PKI 166 hydrochloride

Technical Data
Citations

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.

Solubility for PKI 166 hydrochloride

	Solvent	Max Conc. mM
Solubility
	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.

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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References for PKI 166 hydrochloride

References are publications that support the biological activity of the product.

Ulu 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. 2013 PMID: 23528611
Kaspersen Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena. Bioorg.Chem. 2012 PMID: 22832269
Bruns 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. 2000 PMID: 10850439