过滤
关闭导航

Zidesamtinib [NVL-520],≥98%

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 ROS1 和 ROS1 G2032R 的 IC50 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。
制造商品牌: BSZH
货号(SKU): A19465
CAS号: 2739829-00-4
签订合同 √ 正规发票 √ 技术支持 √ 质量保障 √ 全程可追溯 √
¥9,760.00
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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
NCT NumberSponsorCondition
NCT05118789Nuvalent Inc.
Locally Advanced Solid Tumor|Metastatic Solid Tumor
分子量

419.45

Formula

C22H22FN7O

CAS 号

2739829-00-4

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 20 | 欧洲Eur. ≥ 16 | 東京Tokyo ≥ 5 | 香港与北京 ≥ 20