Formulation: A solid
Formal Name: L-methionyl-L-cysteinyl-L-methionyl-L-prolyl-L-cysteinyl-L-phenylalanyl-L-threonyl-L-threonyl-L-α-aspartyl-L-histidyl-L-glutaminyl-L-methionyl-L-alanyl-L-arginyl-L-lysyl-L-cysteinyl-L-α-aspartyl-L-α-aspartyl-L-cysteinyl-L-cysteinylglycylglycyl-L-lysylglycyl-L-arginylglycyl-L-lysyl-L-cysteinyl-L-tyrosylglycyl-L-prolyl-L-glutaminyl-L-cysteinyl-L-leucyl-L-cysteinyl-L-argininamide, cyclic (2→19),(5→28),(16→33),(20→35)-tetrakis(disulfide), trifluoroacetate salt
Purity: ≥95%
Formula Markup: C158H249N53O47S11 • XCF3COOH
Formula Weight: 3995,7
Shelf life (days): 1460
Notes: Chlorotoxin is a peptide originally isolated from the venom of the scorpion L. quinquestriatus.{72508,72509} It inhibits chloride currents in rat colonic enterocyte plasma membrane preparations when used at a concentration of 594 nM.{72508} Chlorotoxin also binds to, but does not inhibit, matrix metalloproteinase-2 (MMP-2; IC50s = 0.71 and >30 µM, respectively), as well as neuropilin-1 (NRP-1; IC50 = 0.78 µM) in cell-free assays.{72510} It induces paralysis in crayfish (P. clarkii) but is not cytotoxic to human U87MG glioma, MCF-7 breast cancer, PC3 prostate cancer, and A549 lung cancer cells.{72508,72509} Administration of chimeric antigen receptor (CAR) T cells expressing CAR with chlorotoxin as the targeting domain increase survival and decrease tumor volume in an orthotopic patient-derived xenograft (PDX) mouse model of glioblastoma.{72511} Liposomes containing chlorotoxin and encapsulating doxorubicin decrease tumor volume in a U87 glioma mouse xenograft model.{72512} Fluorescently labeled chlorotoxin has been used for tumor imaging in vivo.{72513}
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