AZD3759 (Zorifertinib) hydrochloride is an orally available inhibitor of the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. AZD3759 also inhibits pEGFR in H838wt (IC50: 64.5 nM), H3255L858R (IC50: 7.2 nM), and PC-9exon 19Del (IC50: 7.4 nM), respectively. In cellular phosphorylation studies, AZD3759 also shows 9-fold inhibition selectivity in EGFR-activating mutant cell lines over EGFR wild-type cell lines.
In vivo, AZD3759 (7.5/15 mg/kg) can markedly decrease tumor area. In addition, modulation of pEGFR is detected by a single dose of AZD3759 at 15 mg/kg 1h after dosing.
| Molecular Weight | 496.36 |
| Formula | C22H24Cl2FN5O3 |
| CAS Number | 1626387-81-2 |
| Solubility (25°C) | DMSO ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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