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Zeteletinib hemiadipate
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。
Zeteletinib hemiadipate图片
CAS NO:2375837-06-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
BOS-172738 hemiadipate
DS-5010 hemiadipate
产品介绍
Zeteletinib (BOS-172738; DS-5010) hemiadipate 是一种口服有效的,选择性RET激酶抑制剂,对 RET 具有纳摩尔效力,对 VEGFR2 具有 >300 倍的选择性。Zeteletinib hemiadipate 对野生型RETRETV804M/Lgatekeeper 突变体和最常见的致癌RET突变体M918T显示出较高的效力。Zeteletinib hemiadipate 具有强大的抗肿瘤活性。
生物活性

Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selectiveRETkinaseinhibitor with nanomolar potency againstRETand >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild typeRET,RETV804M/Lgatekeeper mutants, and the most common oncogenicRETmutationM918T. Zeteletinib hemiadipate has potent antitumor activity[1][2][3].

IC50& Target[1]

PDGFR2

 

体外研究
(In Vitro)

In biochemical assays of 106 kinases, RET and platelet-derived growth factor receptor (PDGFR) alpha/beta were inhibited more than 80% by 193 nM Zeteletinib (BOS-172738; DS-5010) hemiadipate. The IC50values of Zeteletinib hemiadipate against RET, RET-GKm (V804L) were single digit nano-molar even under a condition of high concentration of ATP; besides it against KDR was more than 1000 nM[1].

体内研究
(In Vivo)

In biochemical assays of 106 kinases, RET and platelet-derived growth factor receptor (PDGFR) alpha/beta were inhibited more than 80% by 193 nM Zeteletinib (BOS-172738; DS-5010) hemiadipate. The IC50values of Zeteletinib hemiadipate against RET, RET-GKm (V804L) were single digit nano-molar even under a condition of high concentration of ATP; besides it against KDR was more than 1000 nM[1].

Clinical Trial
分子量

573.55

Formula

C25H23F3N4O4.1/2C6H10O4

CAS 号

2375837-06-0

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.