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Gefitinib (hydrochloride)

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Products Details

Product Description

– Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity[1][2].

Web ID

– HY-50895A

Storage Temperature

– 4°C (Powder, sealed storage, away from moisture)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C22H25Cl2FN4O3

Citations

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References

– [1]Wakeling AE, et al. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54.|[2]Moasser MM, et al. The tyrosine kinase inhibitor ZD1839 (“Iressa”) inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8.|[3]Morgillo F, et al. Synergistic effects of metformin treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3508-19.|[4]Miyake K, et al. Epidermal growth factor receptor-tyrosine kinase inhibitor (gefitinib) augments pneumonitis, but attenuates lung fibrosis in response to radiation injury in rats. J Med Invest. 2012;59(1-2):174-85.|[5]Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23.

CAS Number

– 184475-55-6

Molecular Weight

– 483.36

Compound Purity

– 99.85

SMILES

– ClC1=C(C=CC(NC2=NC=NC3=C2C=C(C(OC)=C3)OCCCN4CCOCC4)=C1)F.[H]Cl

Clinical Information

– Launched

Research Area

– Cancer

Solubility

– DMSO : 0.227 mg/mL (ultrasonic;warming)|H2O : 6.25 mg/mL (ultrasonic)

Target

– EGFR

Isoform

– EGFR/ErbB1/HER1

Pathway

– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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