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Chlorotoxin

MCE 国际站：Chlorotoxin

产品活性：Chlorotoxin是从雷蛇属以色列蝎子的毒液中提取的由36个氨基酸组成的肽段，具有抗癌活性。Chlorotoxin是氯离子通道 (chloride channel) 阻断剂。

研究领域：Membrane Transporter/Ion Channel

In Vitro: Chlorotoxin (Chlorotoxin) preferentially binds to tumor cells ａnd has been harnessed to develop an imaging agent to help visualize tumors during surgical resection. In addition, chlorotoxin has potential as a vehicle to deliver anti-cancer drugs specifically to cancer cells. Chlorotoxin is shown to bind glioma cells, but is unable to bind normal rat astrocytes ａnd Te671, a human rhabdomyosarcoma cell line. Chlorotoxin inhibits the migration of U251MG (glioma) cells, with an IC₅₀ of 600 nM. Chlorotoxin binds to glioma cells is specific ａnd involves high affinity (K_d=4.2 nM) ａnd low affinity (K_d=660 nM) binding sites.Small conductance chloride channels are shown to be potently blocked by Chlorotoxin. Chlorotoxin has been used as a general pharmacological tool to investigate the function of chloride channels.

In Vivo: Chlorotoxin shows insecticidal activity on insects ａnd other invertebrates. After the administration of I-Chlorotoxin to tumor-bearing mice, the peptides accumulated within the tumor.Chlorotoxin selectively accumulates in the brain of tumor-bearing mice with calculated brain: muscle ratios of 36.4% of injected dose/g (ID/g), as compared to 12.4%ID/g in control animals.

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