VLX600 是氧化磷酸化(OXPHOS)的铁螯合抑制剂。VLX600 导致线粒体功能障碍，并导致向糖酵解的强烈转变。VLX600 对恶性细胞表现出选择性的细胞毒活性，并诱导自噬 (autophagy)。具有抗癌活性。
| 生物活性 | VLX600 is an iron-chelating inhibitor ofoxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and inducesautophagy. Anticancer activity[1][2]. |
体外研究
(In Vitro) | VLX600 (6 μM; 72 hours) induces an autophagic response[2].
VLX600 is cytotoxic to HCT116 spheroids. VLX600 induces a HIF-1α-dependent glycolytic response. VLX600 inhibits oxygen consumption in HCT116 cells. VLX600 inhibits phosphorylation of the mTOR downstream effectors 4EBP1 and p70-S6K by an HIF-1α-independent mechanism. VLX600 preferentially leads to decreased ATP levels in cancer but not normal cells[2].
Cell Proliferation Assay[2] | Cell Line: | HCT116, HT29, SW620, HT8, DLD and RKO cells | | Concentration: | 0.1, 1, 10, 100μM | | Incubation Time: | 72 hours | | Result: | Inhibited the proliferation of these cells. |
Western Blot Analysis[2] | Cell Line: | HCT116 cells | | Concentration: | 6 μM | | Incubation Time: | 72 hours | | Result: | LC3-II was induced. |
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体内研究
(In Vivo) | VLX600 (16 mg/kg; i.v.; every third day for 16 days) shows anti-tumor activity in human tumor xenografts[2].
| Animal Model: | NMRI nu/nu mice (HCT116 and HT29 colon cancer xenografts)[2] | | Dosage: | 16 mg/kg | | Administration: | Intravenously; every third day for 16 days | | Result: | Anti-tumor activity was observed in both HCT116 and HT29 colon cancer xenografts. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years |
*该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(78.78 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.1511 mL | 15.7555 mL | 31.5110 mL | | 5 mM | 0.6302 mL | 3.1511 mL | 6.3022 mL | | 10 mM | 0.3151 mL | 1.5755 mL | 3.1511 mL |
*请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: 2.08 mg/mL (6.55 mM); Clear solution; Need ultrasonic
此方案可获得 2.08 mg/mL (6.55 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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