Zidesamtinib

Research use only, not for human use.

Zidesamtinib (NVL-520) is an orally active, selective, potent, and blood-brain-barrier-crossing inhibitor of ROS1 fusion and resistance mutations, inhibits ROS1 and ROS1 G2032R, and can be used in the study of non-small-cell lung cancer and solid tumors.

Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer.

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

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.Animal Model:Female athymic Nude-Foxn1nu mice were implanted subcutaneously with tumor fragments from model CTG-0848.Dosage:0.04, 0.2, 1, 5, 15 mg/kg Administration:Oral gavage twice daily for 21 days Result:Inhibited the tumor volumes.

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Immunology/Inflammation

ROS

ROS Kinase

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2739829-00-4

419.455

C22H22FN7O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (119.20 mM; Ultrasonic ( 65°C)

C(C)N1C2=C(CC=3C(C=4C([C@@H](C)OC=5C=C2C=NC5N)=CC(F)=CC4)=NN(C)N3)C=N1

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(-20℃)

With Ice Pack

≥ 2 years