生物活性分子抑制剂VLX600

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VLX600  纯度: 99.35%

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。

VLX600

VLX600 Chemical Structure

CAS No. : 327031-55-0

规格 价格 是否有货 数量
5 mg ￥550 In-stock
10 mg ￥900 In-stock
25 mg ￥1900 In-stock
50 mg ￥3200 In-stock
100 mg ￥5500 In-stock
250 mg ￥11000 In-stock
500 mg   询价  
1 g   询价  

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VLX600 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus

生物活性

VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

317.35

Formula

C17H15N7
CAS 号

327031-55-0
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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 上海金畔生物科技有限公司 网站选购。
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.

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