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AZD3759EGFR inhibitor,oral active

AZD3759

Catalog No. B5962
Size Price Stock Qty
10mM (in 1mL DMSO) $88.00 In stock
5 mg $70.00 In stock
10 mg $100.00 In stock
50 mg $300.00 In stock
100 mg $450.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AZD3759

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Chemical Properties

Cas No. 1626387-80-1 SDF Download SDF
Chemical Name (R)-4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate
Canonical SMILES ClC1=CC=CC(NC2=NC=NC3=CC(OC)=C(OC(N4[C@H](C)CN(C)CC4)=O)C=C23)=C1F
Formula C22H23ClFN5O3 M.Wt 459.90
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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]

Reference:
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