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Gefitinib (ZD1839)Selective EGFR inhibitor

Gefitinib (ZD1839)

Catalog No. A8219
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
Evaluation Sample $28.00 In stock
100mg $105.00 In stock
250mg $190.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Gefitinib (ZD1839)

Related Biological Data

Gefitinib (ZD1839)

Related Biological Data

Gefitinib (ZD1839)

Biological Activity

Description Gefitinib (ZD-1839) is an inhibitor of EGFR for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.
Targets Tyr1173 (NR6wtEGFR cells) Tyr992 (NR6wtEGFR cells) Tyr1173 (NR6W cells) Tyr992 (NR6W cells)    
IC50 37 nM 37nM 26 nM 57 nM    

Protocol

Cell experiment: [1]

Cell lines

BT-474 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

1 μM, 24 hours

Applications

A 24-h treatment of BT-474 cells with 1 μM ZD1839 increased the G1 fraction from 74 to 88% and reduced the proportion of cells in S from 15 to 4%. Simultaneous with the accumulation of cells in G1 was complete elimination of both active Akt and MAPK, as measured with phosphospecific antibodies, without changes in the content of total Akt and MAPK. Consistent with the inhibition of Akt activity, phosphorylation of GSK-3β, a target of the Akt kinase, was reduced. Cyclin D1 and Cdk4 were also reduced, whereas protein levels of the Cdk inhibitor p27 were up-regulated.

Animal experiment: [1]

Animal models

Female Balb/C athymic nude mice injected with BT-474 cells

Dosage form

Oral administration, 200 mg/kg/day

Applications

Mice were randomly allocated to either no treatment, ZD1839, Herceptin, or the combination. ZD1839 completely prevented tumor growth but did not induce complete remissions. Herceptin alone induced complete remission in two of seven, whereas the combination resulted in three of eight complete responses. No mice exhibited treatment-related toxicity. Three mice treated with ZD1839 plus Herceptin, in which tumors regressed completely, remained tumor free for > 6 months after discontinuation of therapy and had no detectable tumor at necropsy.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Moulder S L, Yakes F M, Muthuswamy S K, et al. Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo. Cancer research, 2001, 61(24): 8887-8895.

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Chemical Properties

Cas No. 184475-35-2 SDF Download SDF
Synonyms Iressa,ZD-1839,Gefitinib
Chemical Name N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
Canonical SMILES COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
Formula C22H24ClFN4O3 M.Wt 446.90
Solubility >22.3mg/mL in DMSO Storage Store at -20°C
General tips No
Shipping Condition No

Background

Gefitinib, also known as ZD1839 or Iressa, is a potent and orally-bioavailable small-molecule inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with 50% inhibition concentration IC50 values of 0.033 μM and 0.027 μM in A431 membrane prep and baculovirus lysate respectively. Gefitinib binds to the kinase ATP binding site of EGFR interfering with the binding of adenosine triphosphate, which suppresses the EGFR tyrosine kinase activity and resultant signal transduction of EGFR. Gefitinib exhibits anti-angiogenic activities in a wide range of human tumor types, including head and neck, prostate, breast, ovarian, colon, small-cell lung and non-small-cell lung cancer. Moreover, geftinib has also been found to reduce proliferation, induce cell cycle arrest and increase apoptosis.

Reference

M. Ranson and S. Wardell. Gefitinib, a novel, orally administered agent for the treatment of cancer. Journal of Clinical Pharmacy and Therapeutics (2004) 29, 95-103

Joachim Von Pawel. Gefitinib (Iressa, ZD1839): a novel targeted approach for the treatment of solid tumors. Bull Cancer 2004; 91(5): E70-E76