HKI 357

Key Product Details

Product Description

HKI 357 is a potent, irreversible inhibitor of ErbB2 (HER2) and EGFR (IC₅₀ values are 33 and 34 nM respectively). Suppresses ligand-induced EGFR autophosphorylation and cell proliferation in NCI-H1975 cells containing L858R and T790M mutations. Circumvents mechanisms of resistance to Iressa (Cat. No. 3000) in non-small-cell lung cancer cells.

Product Specifications for HKI 357

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for HKI 357

The following data is based on the product molecular weight 574.05.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

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

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.74 mL	8.71 mL	17.42 mL
5 mM	0.35 mL	1.74 mL	3.48 mL
10 mM	0.17 mL	0.87 mL	1.74 mL
50 mM	0.03 mL	0.17 mL	0.35 mL

Calculators

Background References

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

• Tsou Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity. J.Med.Chem. 2005 PMID: 15715478
• Schiffer Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer. Mol.Pharmacol. 2007 PMID: 16968809
• Kwak Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefi. Proc.Natl.Acad.Sci.USA 2005 PMID: 15897464

Product Documents for HKI 357