VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation, potentiated the effect of radiation in tumor spheroids in a synergistic manner. VLX600 is preferentially active against quiescent cells in colon cancer 3-D microtissues. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation and displays tumour growth inhibition in vivo.
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描述 | VLX600 as a drug that is preferentially active against quiescent cells in colon cancer 3-D microtissues. VLX600 at 0.1 μM -10 μM inhibited the proliferation of HCT116, five additional human colon carcinoma cell lines and two mouse cell lines (T1 breast carcinoma; B16F10 melanoma) in monolayer culture over 72 h, which is associated with induction of autophagy. After exposure of monolayer cells to VLX600, the expression of COX-1, essential for mitochondrial OXPHOS decreased, which was also observed in multicellular spheroids (MCS) core regions. VLX600 induces a HIF-1α-dependent glycolytic response[1]. In vitro, imatinib plus VLX600 at doses higher than 1μM decreased GIST-T1 (Gastrointestinal stromal tumor-T1) cell viability when compared to imatinib or VLX600 alone. In vivo, VLX600 (4.5mg/kg, IV q3–4 days) treatment alone resulted in a significant decrease in GIST-T1 tumor volume compared to vehicle controls[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.15mL 0.63mL 0.32mL |
15.76mL 3.15mL 1.58mL |
31.51mL 6.30mL 3.15mL |
CAS号 | 327031-55-0 |
分子式 | C17H15N7 |
分子量 | 317.348 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 25 mg/mL(78.78 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |