Savolitinib (AZD-6094) 是一种有效的、高选择性的、可口服的 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 竞争性方式选择性结合并抑制 c-Met 的激活，并破坏 c-Met 信号转导通路。抗肿瘤活性。
| Cas No. | 1313725-88-0 |
| 别名 | 赛沃替尼; Volitinib; HMPL-504; AZD-6094 |
| Canonical SMILES | CN1N=CC(C2=CN=C3C(N([C@H](C4=CN5C(C=C4)=NC=C5)C)N=N3)=N2)=C1 |
| 分子式 | C17H15N9 |
| 分子量 | 345.36 |
| 溶解度 | DMSO : ≥ 34 mg/mL (98.45 mM);Water :< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Savolitinib (AZD6094) ia highly potent and selective c-Met inhibitor with an IC50 of 5 nM. References:
[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 development for treatment of cancer. J Med Chem. 2014 Sep 25;57(18):7577-89.
[2]. Schuller A, et al. The MET inhibitor AZD6094 (Savolitinib, HMPL-504) induces regression in papillary renal cell carcinoma patient derived xenograft models. Clin Cancer Res. 2015 Mar 16. pii: clincanres.2685.2014.
[3]. Noh CK, et al. Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS/MS for application to a pharmacokinetic study in rats. J Sep Sci. 2017 Jul 27. |
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