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Zidesamtinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Zidesamtinib图片
CAS NO:2739829-00-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
NVL-520
产品介绍
Zidesamtinib (NVL-520) 是一种有效、选择性,口服活性和可透过血脑屏障的多种ROS1融合和抗性突变抑制剂,对野生型ROS1ROS1 G2032RIC50值分别为 0.7 和 7.9 nM,并且不会抑制 TRK。Zidesamtinib 可用于癌症的研究。
生物活性

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].

体外研究
(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].

体内研究
(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-Foxn1numice 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.
分子量

419.45

Formula

C22H22FN7O

CAS 号

2739829-00-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.