Sunvozertinib (DZD9008) is an effective inhibitor of ErbBs (EGFR, Her2, especially mutants) and BTK. Sunvozertinib showed EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and IC50 of Her2 exon 20 YVMA and EGFR WT A431 They are 20.4, 20.4, 1.1, 7.5 and 80.4 nM respectively (please refer to patent WO2019149164A1, Example 52 for details).
|Solubility (25°C)||DMSO ≥ 60 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Mengzhao Wang, et al. Cancer Discov. Sunvozertinib, a selective EGFR inhibitor for previously treated non-small cell lung cancer with EGFR exon 20 insertion mutations
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