HKI 357

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Cat.No. 3580 - HKI 357 | C31H29ClFN5O3 | CAS No. 848133-17-5
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
Literature

Biological Activity

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.

Compound Libraries

HKI 357 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 57.4 100
ethanol 14.35 25

Preparing Stock Solutions

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

Molarity Calculator

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Reconstitution Calculator

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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.

Kwak et al (2005) Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. 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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Keywords: HKI357 EGFR epidermal growth factor receptors inhibitors inhibits irreversible dual potent ErbB2 HER2 EGFR

Citations for HKI 357

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Literature in this Area

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Pathways for HKI 357

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