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Catalog No.
EGFR inhibitor,oral active
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
5 mg
In stock
10 mg
In stock
50 mg
In stock
100 mg
In stock

Tel: +1-832-696-8203

Email: [email protected]

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AZD3759 is a potent and oral active inhibitor of EGFR (IC50= 7.0-7.7 nM) with antineoplastic activity.

EGFR (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc.

AZD3759 shows equally potent inhibitory effect on cell phosphorylation or proliferation in EGFR-activating mutant cell lines (PC-9 and H3255) in the range of 7.0−7.7nM. In cellular phosphorylation assays, AZD3759 also exhibits 9-fold inhibition selectivity in EGFR-activating

mutant cell lines over EGFR wild-type cell lines (H838). [1]

In brain metastasis mouse model, AZD3759 demonstrates prominent antitumor efficacy in a dose dependent manner (∼78% tumor growth inhibition at 7.5 mg/kg qd and tumor regression at 15 mg/kg qd, respectively, 4 weeks after treatment, with <20% body weight loss). In addition, at the doses of 7.5 and 15 mg/k, AZD3759 significantly decreases tumor area in the brain tissue collected from the same mouse model. [1]

Zeng Q, Wang J, Cheng Z et al.  Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Oct 22;58(20):8200-15

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.1626387-80-1
Solubility≥23mg/mL in DMSO
Chemical Name(R)-4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate
SDFDownload SDF
Canonical SMILESClC1=CC=CC(NC2=NC=NC3=CC(OC)=C(OC(N4[[email protected]](C)CN(C)CC4)=O)C=C23)=C1F
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Chemical structure