GW 583340 dihydrochloride

Name: GW 583340 dihydrochloride
Brand: Tocris Bioscience
SKU: 2239

Tocris Bioscience, part of Bio-Techne | Catalog # 2239

Citations (1)

COA / SDS

Potent dual EGFR/ErbB2 inhibitor; orally active

Key Product Details

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)
Molecular Weight:	671.03

View Full Technical Details for GW 583340 dihydrochloride

Technical Data
Citations

Biological Activity for GW 583340 dihydrochloride

GW 583340 dihydrochloride is a 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 for GW 583340 dihydrochloride

GW 583340 dihydrochloride is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for GW 583340 dihydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GW 583340 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	67.1	100 with gentle warming

Preparing Stock Solutions for GW 583340 dihydrochloride

The following data is based on the product molecular weight 671.03.

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	1.49 mL	7.45 mL	14.90 mL
5 mM	0.30 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	0.30 mL

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References for GW 583340 dihydrochloride

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

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