PKI 166 hydrochloride

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Cat.No. 4941 - PKI 166 hydrochloride | C20H18N4O.HCl
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)
Datasheet
Citations

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
Storage Store at +4°C
Purity ≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble 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.

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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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Keywords: 187724-61-4 potent EGFR kinase inhibitors epidermal growth factor receptor tyrosine antiangiogenic antitumor antitumour inhibits PKI166 EGFR

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