| 产品描述: | OXPHOS 抑制剂;OXPHOS Inhibitors;;InformationVLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS) , potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.TargetsOXPHOSIn vitroVLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. Mitochondrial inhibition with VLX600 has a direct antitumor effect in vitro while appearing to promote glycolysis through increased AKT signaling and glucose transporter expression. When combined with imatinib, VLX600 prevents imatinib-induced cell cycle escape and reduces p27 expression, leading to increased apoptosis when compared to imatinib alone.In vivoVLX600 induces the formation of autolysosomes in vivo. VLX600 displays tumour growth inhibition in vivo. When combined with imatinib, VLX600 reduces p27 expression and prevents imatinib-induced cell cycle escape, likely potentiating the antitumoral effects of Kit inhibition.Cell Research(from reference)Cell lines:human GIST-T1 cell line, human HG129 cell line, human GIST-882 cell line, Concentrations:2 μM, 6 μM, 12 μM Incubation Time:48–72h |
| 体内研究: |
VLX600 (16 mg/kg;静脉注射;每三天一次,持续 16 天) 在肿瘤异种移植瘤模型中显示出抗肿瘤活性。 |
| 参考文献: |
1. Karlsson H, et al. A novel tumor spheroid model identifies selective enhancement of radiation by an inhibitor of oxidative phosphorylation. Oncotarget. 2019 Sep 3;10(51):5372-5382. 2. Zhang X, et al. Induction of mitochondrial dysfunction as a strategy for targeting tumour cells in metabolically compromised microenvironments. Nat Commun. 2014;5:3295. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.151 ml |
15.755 ml |
31.511 ml |
| 5 mM |
0.63 ml |
3.151 ml |
6.302 ml |
| 10 mM |
0.315 ml |
1.576 ml |
3.151 ml |
| 50 mM |
0.063 ml |
0.315 ml |
0.63 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。 |