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AZD3759

Cat. No. M5164

All AbMole products are for research use only, cannot be used for human consumption.

AZD3759 Structure
Synonym:

Zorifertinib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 30  USD30 In stock
10mg USD 40  USD40 In stock
50mg USD 85  USD85 In stock
100mg USD 137  USD137 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Chemical Information
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
References

[1] Zeng Q, et al. J Med Chem. Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.

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Keywords: AZD3759, Zorifertinib supplier, EGFR/HER2, inhibitors, activators

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