99% Purity AZD3759 Powder for Cancer treatment 1626387-80-1
English name: AZD 3759
English Synonyms: AZD 3759; AZD3759; AZD-3759; (2R) -2,4-Dimethyl-
1-piperazinecarboxylic acid 4 - [(3-chloro-2- fluorophenyl) amino]
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
Patients with meningeal metastases from this clinical trial benefit
from the treatment of AZD3759, and the
300 mg dose appears to achieve greater control.
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
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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