Zorifertinib (AZD3759) is an orally bioavailable, brain-penetrant epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed specifically to treat non-small cell lung cancer (NSCLC) with EGFR-activating mutations and central nervous system (CNS) metastases. It exhibits high potency against mutant EGFR, particularly the L858R and exon 19 deletion variants, with in vitro IC₅₀ values in the low nanomolar range (e.g., ~5–10 nM for EGFR-L858R). Notably, AZD3759 achieves cerebrospinal fluid (CSF) concentrations sufficient to inhibit intracranial tumor growth, a limitation of earlier EGFR TKIs. In preclinical models, it demonstrated robust antitumor activity in both intracranial and extracranial xenografts.
MedKoo Cat#: 575206
Name: Zorifertinib HCl
CAS#: 1626387-81-2 (HCl)
Chemical Formula: C22H24Cl2FN5O3
Exact Mass: 495.1240
Molecular Weight: 496.36
Elemental Analysis: C, 53.24; H, 4.87; Cl, 14.28; F, 3.83; N, 14.11; O, 9.67
The following data is based on the product molecular weight 496.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
