China Supply 9% Purity AZD 3759 CAS: 1626387-80-1 for Cancer Treatment

Item No.: 1626387-80-1
Model NO.: 1626387-80-1
Customized: Non-Customized
Suitable for: Elderly, Adult
Purity: >99%
Delivery Time: 4-7 Days
Transport Package: Foil Bag or Tin. &Well Disguised Package with Fast
Certification: GMP, ISO 9001
Appearance: White or off-White C
Quick Details:

English name: AZD 3759
English Synonyms: AZD 3759; AZD3759; AZD-3759; (2R) -2,4-Dimethyl- 1-piperazinecarboxylic acid 4 - [(3-chloro-2- fluorophenyl) amino] HY-18750; azd3579;
CAS number: 1626387-80-1
Molecular formula: C22H23ClFN5O3
Molecular weight: 459.91


AZD3759 is a potent, orally active, CNS-permeable EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del, . AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 showed an inhibitory effect on the proliferation of PC-9 and H3255 cells derived from the pEGFR pathway and the EGFR mutant with IC50 of 7.7 nM and 7 nM, respectively, with no activity on the proliferation of H838 cells.
Phase 1 clinical trials of AZD3759 showed very good control activity of intracranial lesions, and the dose of this drug is recommended to be 200 mg or 300 mg twice daily. AZD3759 has no better control of extracranial lesions than the other EGFR-targeted agents, but shows greater control over intracranial lesions.


1.Non-small cell lung cancer is one of the major diseases that threaten human health. Even more serious is up to 50% of cancer patients with central nervous system metastasis in their lifetime, metastatic lung cancer is currently no cure. Recently, AstraZeneca's Chinese team led by Dr. Zhang Xiaolin successfully developed a new drug, AZD3759, to treat central nervous system metastases of lung cancer. Their early R & D results have been published in "Journal of Medicinal Chemistry".

2.In order to solve the challenging problem of blood-brain barrier, the author comprehensively optimizes structural parameters such as molecular size, polarity, rigidity and the like, and adjusts various biophysical and chemical properties such as basicity, water solubility, permeability and stability To the best condition to cross the blood-brain barrier. The fully optimized design has successfully brought AZD3759 to the same effective concentrations in different settings of the blood and central nervous system. In addition, the authors also published a preclinical in vitro and in vivo assessment of a subset of candidate compounds. Clinical studies of AZD3759 are underway.

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