Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverseROS1 fusionsandresistance mutations, withIC₅₀s of 0.7 and 7.9 nM forwild-type ROS1andROS1 G2032R, respectively, and sparesTRKinhibition. Zidesamtinib can be used for the research ofcancer^[1].

Zidesamtinib (72 h) inhibits the growth of seven cell lines expressing wild-type ROS1 fusions, with average IC₅₀s of 0.4 nM^[1].
Zidesamtinib (72 h) inhibits the growth of six cell lines harboring ROS1 fusions with the G2032R mutation, with average IC₅₀s of 1.6 nM^[1].
Zidesamtinib (72 h) potently inhibits the non-G2032R ROS1 mutants, with IC₅₀s ≤ 1.5 nM^[1].
Zidesamtinib (10-1000 nM; 4 weeks) suppresses colony formation in NIH3T3 cells expressing wild-type ROS1 fusions and expressing ROS1 fusions with G2032R^[1].

Zidesamtinib (0.04-15 mg/kg; p.o. twice daily for 28 d) induces tumor regression at all doses ≥0.2 mg/kg in wild-type ROS1 xenograft models^[1].

419.45

C₂₂H₂₂FN₇O

2739829-00-4

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