VLX600是一种新型的铁螯合剂,抑制氧化磷酸化,增强辐射对肿瘤球体的效果,具有协同作用。VLX600在结肠癌3D微组织中的静止细胞中表现出优先活性,并在营养缺乏条件下显示出增强的细胞毒活性,表现出体内肿瘤生长抑制。
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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 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,Room temperature |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |