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Submit ReviewHKI 357
Description: Dual irreversible inhibitor of ErbB2 and EGFR
Chemical Name: (2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Purity: ≥98% (HPLC)
Biological Activity for HKI 357
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.
Technical Data for HKI 357
| M. Wt | 574.05 |
| Formula | C31H29ClFN5O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 848133-17-5 |
| PubChem ID | 11238512 |
| InChI Key | NERXPXBELDBEPZ-RMKNXTFCSA-N |
| Smiles | O=C(/C=C/CN(C)C)NC1=C(OCC)C=C(N=CC(C#N)=C2NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1 |
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 HKI 357
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.4 | 100 | |
| ethanol | 14.35 | 25 |
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 will affect the solvent volumes required to prepare stock solutions.
| 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 |
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Product Datasheets for HKI 357
References for HKI 357
References are publications that support the biological activity of the product.
Kwak et al (2005) Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefi. Proc.Natl.Acad.Sci.USA 102 7665 PMID: 15897464
Tsou et al (2005) 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. 48 1107 PMID: 15715478
Schiffer et al (2007) Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer. Mol.Pharmacol. 71 508 PMID: 16968809
If you know of a relevant reference for HKI 357, please let us know.
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Keywords: HKI 357, HKI 357 supplier, HKI357, EGFR, epidermal, growth, factor, receptors, inhibitors, inhibits, irreversible, dual, potent, ErbB2, HER2, 3580, Tocris Bioscience
Citations for HKI 357
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