| 产品描述: | LY2334737 is an nucleoside analog and is an orally active proagent of Gemcitabine. LY2334737 exhibits inhibitory activity against enterovirus A71 (EV-A71) infection. LY2334737 has antiviral and anticancer effects |
| 靶点: |
Enterovirus A71 (EV-A71);NucleosideAntimetabolite/Analog;Others;VirusProtease |
| 体外研究: |
Five cell lines that express CES2 responded to LY2334737 treatment. LY2334737 is less cytotoxic to a SK-OV-3 CES2 knockdown than parental cells. The drug response of CES2-transfected HCT-116 cells correlated with CES2 expression level. Bystander studies show statistically greater PC-3-GFP growth inhibition by LY2334737 when cells are cocultured with CES2 and not mock transfectants |
| 体内研究: |
Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once a day for 21 days shows greater tumor growth inhibition of CES2 transfectant than the mock transfectant. Metronomic LY2334737 administration causes increased blood flow in luciferase-tagged LM2-4 tumor xenografts, and this effect, readily measured using contrast micro-ultrasound, coincided with a relative increase in tumor bioluminescence |
| 参考文献: |
1. Pratt SE, et al. Human carboxylesterase-2 hydrolyzes the prodrug of gemcitabine (LY2334737) and confers prodrug sensitivity to cancer cells. Clin Cancer Res. 2013 Mar 1;19(5):1159-68. 2. Jialei Sun, et al. Drug Repurposing of Pyrimidine Analogs as Potent Antiviral Compounds Against Human Enterovirus A71 Infection With Potential Clinical Applications. Sci Rep. 2020 May 18;10(1):8159. 3. Francia G, et al. Low-dose metronomic oral dosing of a prodrug of gemcitabine (LY2334737) causes antitumor effects in the absence of inhibition of systemic vasculogenesis. Mol Cancer Ther. 2012 Mar;11(3):680-9. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.568 ml |
12.84 ml |
25.681 ml |
| 5 mM |
0.514 ml |
2.568 ml |
5.136 ml |
| 10 mM |
0.257 ml |
1.284 ml |
2.568 ml |
| 50 mM |
0.051 ml |
0.257 ml |
0.514 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |