1. Protein Tyrosine Kinase/RTK
  2. RET PDGFR
  3. Zeteletinib hemiadipate

Zeteletinib hemiadipate  (Synonyms: BOS-172738 hemiadipate; DS-5010 hemiadipate)

目录号: HY-139590A
产品使用指南

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/L gatekeeper 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。

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Zeteletinib hemiadipate Chemical Structure

Zeteletinib hemiadipate Chemical Structure

CAS No. : 2375837-06-0

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  • 生物活性

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  • 参考文献

生物活性

Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. 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 IC50 values 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].

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

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 IC50 values 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].

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

Clinical Trial
分子量

573.55

Formula

C25H23F3N4O4.1/2C6H10O4

CAS 号
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.

纯度 & 产品资料
参考文献

Zeteletinib hemiadipate 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
HY-139590A
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