GW 583340 dihydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 2239 - GW 583340 dihydrochloride | C28H25ClFN5O3S2.2HCl | CAS No. 1173023-85-2
Description: Potent dual EGFR/ErbB2 inhibitor; orally active
Chemical Name: N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[2-[[[2-(methylsulfonyl)ethyl]amino]methyl]-4-thiazolyl]-4-quinazolinamine dihydrochloride
Purity: ≥97% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 values are 0.01 and 0.014 μM respectively). Selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50 values are 0.11 μM for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μM for inhibition of non-tumor cell line HFF). Inhibits tumor growth in vivo by ~ 80% in a murine xenograft model following oral administration.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Compound Libraries

GW 583340 dihydrochloride 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 671.03
Formula C28H25ClFN5O3S2.2HCl
Storage Desiccate at +4°C
Purity ≥97% (HPLC)
CAS Number 1173023-85-2
PubChem ID 16219404
InChI Key WIMITXDBYLKRKB-UHFFFAOYSA-N
Smiles Cl.Cl.CS(=O)(=O)CCNCC1=NC(=CS1)C1=CC=C2N=CN=C(NC3=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 67.1 100mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 671.03. 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 1.49 mL 7.45 mL 14.9 mL
5 mM 0.3 mL 1.49 mL 2.98 mL
10 mM 0.15 mL 0.75 mL 1.49 mL
50 mM 0.03 mL 0.15 mL 0.3 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.

Gaul et al (2003) Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines. Bioorg.Med.Chem.Lett. 13 637 PMID: 12639547


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Keywords: Potent dual EGFR ErbB2 inhibitors inhibits orally active Epidermal Growth Factors Receptors Her Receptor Tyrosine Kinases RTKs GW583340 dihydrochloride GlaxoSmithKline GSK EGFR

Citations for GW 583340 dihydrochloride

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Literature in this Area

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Cancer Research Product Guide

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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