2739829-00-4
2739829-00-4 structure
- Name: Zidesamtinib
- Chemical Name: Zidesamtinib
- CAS Number: 2739829-00-4
- Molecular Formula: C22H22FN7O
- Molecular Weight: 419.45
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK ROS
- Create Date: 2023-04-14 16:53:20
- Modify Date: 2024-04-07 12:37:18
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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[1].
| Name | Zidesamtinib |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| In Vitro | 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]. |
| In Vivo | 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]. Animal Model: Female athymic Nude-Foxn1nu mice were implanted subcutaneously with tumor fragments from model CTG-0848[1] Dosage: 0.04, 0.2, 1, 5, 15 mg/kg Administration: Oral gavage twice daily for 21 days Result: Inhibited the tumor volumes. |
| References |
| Molecular Formula | C22H22FN7O |
|---|---|
| Molecular Weight | 419.45 |