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1626387-80-1 AZD3759 AZD-3759
Chinese Name: AZD3759
English Name: AZD3759
English alias: 4 - ((3-chloro-2-fluorophenyl) amino) - 7-methoxyquinazolin-6-yl (2R) - 2,4-dimethylpiperazine-1-carboxylate; (R) - 4 - ((3-chloro-2-fluorophenyl) amino) - 7-methoxynazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate;
CAS: 1626387-80-1
Molecular formula: C22H23ClFN5O3
Molecular weight: 459.90100
Exact mass: 459.14700 PSA:79.82000 LogP:4.25800
Appearance and character: white or gray solid.
Melting point: 192.4 degrees C (alcohol, ester), 193.3 degree C (water)
Water solubility: soluble in DMSO
Content: more than 99% pharmaceutical grade
AZD3759 has a very high passive permeability (29.5x10-6 cmc), not a substrate of transmembrane glycoprotein (Pgp), but Kpuu, brain and Kpuu, CSF > 0.5 in immune mice and monkeys.
Preliminary clinical results: Four patients with brain-to-brain NSCLC, three patients with 50 mg*2 per day and one patient with 100 mg*2 per day. Among them, two patients were assessable and one patient was stable. The drug concentration in CSF was 7.7nM and 6nM, approximately equal to the pEGFR IC50 of AZD3759. No side effects were found in the clinic.
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