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AZD3759 (Zorifertinib) is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively.
AZD3759 (Zorifertinib) inhibits EGFR phosphorylation with IC50 of 7.2 nM in H3255 (L858R) cells. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively.
In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy. AZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain.
Biomed Pharmacother. 2024 Jun 21.
The combination therapy using tyrosine kinase receptors inhibitors and repurposed drugs to target patient-derived glioblastoma stem cells
AZD3759 purchased from AbMole
Bioengineered. 2022 Jan;13(1):331-344.
AZD3759 enhances radiation effects in non-small-cell lung cancer by a synergistic blockade of epidermal growth factor receptor and Janus kinase-1
AZD3759 purchased from AbMole
Bioengineered. 2021 Dec;12(1):8679-8689.
AZD3759 inhibits glioma through the blockade of the epidermal growth factor receptor and Janus kinase pathways
AZD3759 purchased from AbMole
| Molecular Weight | 459.9 |
| Formula | C22H23ClFN5O3 |
| CAS Number | 1626387-80-1 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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Products are for research use only. Not for human use. We do not sell to patients.
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