赛沃替尼 /Savolitinib
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货号：A569590
同义名：
赛沃替尼（AZD6094）
/ Volitinib;HMPL-504
Savolitinib is an orally bioavailable inhibitor of the c-Met receptor tyrosine kinase (IC50= 5 nM) with potential antineoplastic activity.
Savolitinib 化学结构
Savolitinib 3D分子结构
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Savolitinib 纯度/质量文件 产品仅供科研
货号：A569590
标准纯度：
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Savolitinib 质控信息
Savolitinib 生物活性
描述
Savolitinib is a novel triazolopyrazine-based c-Met inhibitor with IC50 values of 5nM, 3nM and 6nM for inhibition of c-Met enzyme, HGF-mediated c-Met phosphorylation and HGF-induced proliferation assay in NCI-H441 cell line, respectively. Single oral dose of 3 mg/kg Savolitinib achieved inhibition of HGF-mediated c-Met phosphorylation by 84.7% at 6h post administration in mice. Oral dose of savolitinib at 1, 2.5 and 10mg/kg once daily for 21 days dose-dependently inhibited tumor growth in U87MG subcutaneous xenograft athymic nude mice model[1] [2]
作用机制
Savolitinib can bind to c-Met in a unique mode including wrapping around Met1211 c-Met in a“U-shaped” conformation. It also binds to the activation loop through Asp1228 and Lys1110 residues.[1] [2]
Savolitinib 动物研究
Dose
Mice: 0.3 mg/kg - 10 mg/kg[3] [4] [3]
Administration
p.o., i.v.
Pharmacokinetics
Animal
Mice[1]
Dose
2.5 mg/kg (i.v.)
Administration
i.v.
F
27.2% (p.o.)
T1/2
1.7 h (p.o.)
Vz
1.2 l/kg (i.v.)
CLp
0.66 l/h·kg (i.v.)
Cmax
4947 ng/ml (p.o.)
AUC0→8h
5594 ng·h/ml (p.o.)
Savolitinib 参考文献
[1] Jia H, Dai G, 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 development for treatment of cancer. J Med Chem. 2014 Sep 25;57(18):7577-89.
[2] Bahcall M, Sim T, et al. Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer. Cancer Discov. 2016 Dec;6(12):1334-1341. Epub 2016 Sep 30.
[3] Gavine PR, Ren Y, 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.
[4] Henry RE, Barry ER, et al. Acquired savolitinib resistance in non-small cell lung cancer arises via multiple mechanisms that converge on MET-independent mTOR and MYC activation. Oncotarget. 2016 Sep 6;7(36):57651-57670.
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Savolitinib 实验方案
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存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.90mL
0.58mL
0.29mL
14.48mL
2.90mL
1.45mL
28.96mL
5.79mL
2.90mL
Savolitinib 技术信息
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