Savolitinib|1313725-88-0|(赛沃替尼; Volitinib; HMPL-504; AZD-6094)-陌孚医药/Medlife

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Savolitinib (Synonyms: 赛沃替尼; Volitinib; HMPL-504; AZD-6094)

目录号: PL04568 纯度: ≥99%

CAS No. :1313725-88-0

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中文名称	Savolitinib
中文别名	沃利替尼;Savolitinib;赛沃替尼
英文名称	Savolitinib
英文别名	Volitinib;AZD-6094;HMPL-504;1-[(1S)-1-Imidazo[1,2-a]pyridin-6-ylethyl]-6-(1-methyl-1H-pyrazol-4-yl)-1H-1,2,3-triazolo[4,5-b]pyrazine;Savolitinib;AZD6094;HMPL504;2A2DA6857R;(S)-1-(1-(imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine;3-[(1S)-1-imidazo[1,2-a]pyridin-6-ylethyl]-5-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyrazine;Savolitinib [INN];Volitinib(Savolitinib);Savolitinib (USAN/INN);Savolitinib [USAN:INN];GTPL9918;HMPL 504;AZD 6094;BDBM50023342;NSC782121
Cas No.	1313725-88-0
分子式	C₁₇H₁₅N₉
分子量	345.36
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Savolitinib (AZD-6094) 是一种高效选择性、口服生物利用度 c-Met 抑制剂，对 c-Met 和 p-Met 的 IC₅₀ 分别为 5 nM 和 3 nM。Savolitinib (AZD-6094) 以 ATP 竞争的方式选择性结合并抑制 c-Met 的激活，破坏 c-Met 信号转导途径。具有抗肿瘤活性。

生物活性

Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC 50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity.

性状

Solid

IC50 & Target[1][2]

IC50: 5 nM (c-Met) and 3 nM (p-Met)

体内研究(In Vivo)

Savolitinib (Compound 28; 1-10.0 mg/kg; oral administration; daily; for 21 days; athymic nude mice) demonstrates dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model. In addition, none of the mice in the dosing groups exhibits body weight loss during the experiment. 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]. Jia H, et al. Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical devel
[2]. Gavine PR, et al. Volitinib, a potent and highly selective c-Met inhibitor, effectively blocks c-Met signaling and growth in c-MET amplified gastric cancer patient-derived tumor xenograft models. Mol Oncol. 2015 Jan;9(1):323-33.

溶解度数据	In Vitro: DMSO : ≥ 20.83 mg/mL (60.31 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

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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