产品
编 号：F755150
分子式：C22H22FN7O
分子量：419.45
分子式：C22H22FN7O
分子量：419.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
结构图
CAS No: 2739829-00-4
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 (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.
体内研究：
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.
体外研究：
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.
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