GW 583340 dihydrochloride

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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 (1)
Reviews
Literature (4)

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 Kinase Inhibitor Library. 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.

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 67.1 100 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 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 1.49 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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References

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

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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View all EGFR Inhibitors

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1 Citation for GW 583340 dihydrochloride

Citations are publications that use Tocris products. Selected citations for GW 583340 dihydrochloride include:

Sodani et al (2012) GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. Biochem Pharmacol 83 1613 PMID: 22414725


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