CAS 163515-35-3|Chlorotoxin TFA
| Common Name | Chlorotoxin TFA | ||
|---|---|---|---|
| CAS Number | 163515-35-3 | Molecular Weight | 3995.70000 |
| Density | / | Boiling Point | / |
| Molecular Formula | C158H249N53O47S11 | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | / |
Names
| Name | Chlorotoxin |
|---|---|
| Synonym | More Synonyms |
Chlorotoxin TFA BiologicalActivity
| Description | 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. |
|---|---|
| Related Catalog | Signaling Pathways >>Membrane Transporter/Ion Channel >>Chloride ChannelResearch Areas >>CancerPeptides |
| Target | Target: Chloride Channel[1] |
| 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]. |
| 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]. |
| Animal Admin | 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]. |
| References | [1]. DeBin JA, et al. Purification and characterization of chlorotoxin, a chloride channel ligand from the venom of the scorpion. Am J Physiol. 1993 Feb;264(2 Pt 1):C361-9. [2]. Ojeda PG, et al. Chlorotoxin: Structure, activity, and potential uses in cancer therapy. Biopolymers. 2016 Jan;106(1):25-36. [3]. Soroceanu L, et al. Use of chlorotoxin for targeting of primary brain tumors. Cancer Res. 1998 Nov 1;58(21):4871-9. [4]. Dardevet L, et al. Chlorotoxin: a helpful natural scorpion peptide to diagnose glioma and fight tumor invasion. Toxins (Basel). 2015 Mar 27;7(4):1079-101. |
Chemical & Physical Properties
| Molecular Formula | C158H249N53O47S11 |
|---|---|
| Molecular Weight | 3995.70000 |
| Exact Mass | 3992.50000 |
| PSA | 2001.75000 |
| InChIKey | QPAKKWCQMHUHNI-XUJKACQMSA-N |
| SMILES | CSCCC(N)C(=O)NC1CSSCC2NC(=O)C(CC(=O)O)NC(=O)C(CC(=O)O)NC(=O)C3CSSCC4NC(=O)C(CCC(N)=O)NC(=O)C5CCCN5C(=O)CNC(=O)C(Cc5ccc(O)cc5)NC(=O)C(CSSCC(NC(=O)C5CCCN5C(=O)C(CCSC)NC1=O)C(=O)NC(Cc1ccccc1)C(=O)NC(C(C)O)C(=O)NC(C(C)O)C(=O)NC(CC(=O)O)C(=O)NC(Cc1c[nH]cn1)C(=O)NC(CCC(N)=O)C(=O)NC(CCSC)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)N3)NC(=O)C(CCCCN)NC(=O)CNC(=O)C(CCCNC(=N)N)NC(=O)CNC(=O)C(CCCCN)NC(=O)CNC(=O)CNC(=O)C(CSSCC(C(=O)NC(CCCNC(=N)N)C(N)=O)NC(=O)C(CC(C)C)NC4=O)NC2=O |
| Storage condition | -20°C |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
Articles2
More Articles| Purification and characterization of chlorotoxin, a chloride channel ligand from the venom of the scorpion. Am. J. Physiol. 264 , C361, (1993) We have previously demonstrated that the venom of the scorpion Leiurus quinquestriatus blocks small-conductance Cl- channels, derived from epithelial cells, when applied to the cytoplasmic surface. We... | |
| Expression of voltage-activated chloride currents in acute slices of human gliomas. Neuroscience 83 , 1161-1173, (1998) Using whole-cell patch-clamp recordings, we identified a novel voltage-activated chloride current that was selectively expressed in glioma cells from 23 patient biopsies. Chloride currents were identi... |
Synonyms
| 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 |
