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Chlorotoxin
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。
Chlorotoxin Chemical Structure
CAS No. : 163515-35-3
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生物活性 |
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker. |
IC50 & Target |
Target: Chloride Channel[1] |
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体外研究 (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[2]. Chlorotoxin binds to glioma cells is specific and involves high affinity (Kd=4.2 nM) and low affinity (Kd=660 nM) binding sites[3].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[4]. 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. |
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体内研究 (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[2].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[3]. 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. |
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Clinical Trial |
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分子量 |
3995.71 |
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Formula |
C158H249N53O47S11 |
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CAS 号 |
163515-35-3 |
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Sequence |
Met-Cys-Met-Pro-Cys-Phe-Thr-Thr-Asp-His-Gln-Met-Ala-Arg-Lys-Cys-Asp-Asp-Cys-Cys-Gly-Gly-Lys-Gly-Arg-Gly-Lys-Cys-Tyr-Gly-Pro-Gln-Cys-Leu-Cys-Arg-NH2 (Disulfide bridge: Cys2-Cys19,Cys5-Cys28,Cys16-Cys33,Cys20-Cys35) |
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Sequence Shortening |
MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR-NH2 (Disulfide bridge: Cys2-Cys19,Cys5-Cys28,Cys16-Cys33,Cys20-Cys35) |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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参考文献 |
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Animal Administration [3] |
Mouse: At 24, 48, 72, and 96 h after tumor-bearing and control SCID mice are injected with 125l-labeled Chlorotoxin, they are anesthetized and imaged. Both 125I- and 131l-labeled Chlorotoxin-injected animals and their control counterparts are killed at indicated time points for biodistribution studies[3]. 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. |
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参考文献 |
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