Zeteletinib|2216753-97-6|(BOS-172738; DS-5010)-陌孚医药/Medlife

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

目录号: PL08987 纯度: ≥99%

CAS No. :2216753-97-6

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中文名称	Zeteletinib
英文名称	Zeteletinib
英文别名	Zeteletinib;EP0P7SHM0U;BOS172738;DS5010;Zeteletinib [INN];BOS172738 free base;GTPL11416;US10851092, Example 3;BDBM475603;Example 3 [WO2018060714A1];2-(6-(6,7-Dimethoxyquinolin-3-yl)pyridine-3-yl))-N-(3-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-5-yl)acetamide;2-[6-(6,7-dimethoxyquinolin-3-yl)pyridin-3-yl]-N-[3-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-5-yl]acetamide;3-Pyridinea
Cas No.	2216753-97-6
分子式	C₂₅H₂₃F₃N₄O₄
分子量	500.47
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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、RET^V804M/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。

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, RET gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity.

性状

Solid

IC50 & Target[1][2]

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

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

ClinicalTrial

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) 3

溶解度数据	In Vitro: DMSO : 100 mg/mL (199.81 mM; Need ultrasonic)配制储备液

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Data Sheet

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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