HKI 357

Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (4)

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.

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

Certificate of Analysis / Product Datasheet
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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


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Citations for HKI 357

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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