标签归档：zeteletinib

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

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Zeteletinib (Synonyms: BOS-172738; DS-5010) 纯度: 99.06%

Zeteletinib (BOS-172738; DS-5010) 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 对野生型 RET、RETV804M/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 具有强大的抗肿瘤活性。

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

Zeteletinib Chemical Structure

CAS No. : 2216753-97-6

规格 价格 是否有货 数量
5 mg ￥8500 In-stock
10 mg ￥13500 In-stock
50 mg   询价  
100 mg   询价  

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Zeteletinib 相关产品

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  • Bioactive Compound Library Plus

生物活性

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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In a Ba/F3-RET subcutaneous tumor model, Zeteletinib (BOS-172738; DS-5010) dosing at 10 mg/kg twice daily (bid) induces tumor regression[1].
In an LC2/ad NSCLC xenograft model, which has the RET-CCDC6 fusion gene, Zeteletinib dosing at 1 mg/kg thrice daily (tid) induced tumor regression[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

500.47

Formula

C25H23F3N4O4
CAS 号

2216753-97-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Yasuyuki Kaneta, et al.Abstract B173: Preclinical characterization and antitumor efficacy of DS-5010, a highly potent and selective RET inhibitor. MOLECULAR CANCERTHERAPEUTICS. January 2018, Volume 17, Issue 1.

    [2]. Patrick Schoffski, et al. BOS172738, a highly potent and selective RET inhibitor, for the treatment of RET-altered tumors including RET-fusion+ NSCLC and RET-mutant MTC: Phase 1 study results. Journal of Clinical Oncology 39, no. 15_suppl (May 20, 2021) 3008-3008.

    [3]. Kyaw Z Thein, et al. Precision therapy for RET-altered cancers with RET inhibitors. Trends Cancer. 2021 Dec;7(12):1074-1088.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

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

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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

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 RET、RETV804M/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。

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

Zeteletinib hemiadipate Chemical Structure

CAS No. : 2375837-06-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Zeteletinib hemiadipate 的其他形式现货产品:

Zeteletinib

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].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

573.55

Formula

C31H33F3N4O8
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.
参考文献

  • [1]. Yasuyuki Kaneta, et al.Abstract B173: Preclinical characterization and antitumor efficacy of DS-5010, a highly potent and selective RET inhibitor. MOLECULAR CANCERTHERAPEUTICS. January 2018, Volume 17, Issue 1.

    [2]. Patrick Schoffski, et al. BOS172738, a highly potent and selective RET inhibitor, for the treatment of RET-altered tumors including RET-fusion+ NSCLC and RET-mutant MTC: Phase 1 study results. Journal of Clinical Oncology 39, no. 15_suppl (May 20, 2021) 3008-3008.

    [3]. Kyaw Z Thein, et al. Precision therapy for RET-altered cancers with RET inhibitors. Trends Cancer. 2021 Dec;7(12):1074-1088.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务