Gly-Gly-Phe-Gly-NH-O-CO-Exatecan hydrochloride

• CAT Number: I040115
• Molecular Formula: C42H46ClFN8O10
• Molecular Weight: 877.31
• Purity: ≥95%
• Synonyms: (2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-N-[2-[[2-[[(10S,23S)-10-ethyl-18-fluoro-10-hydroxy-19-methyl-5,9-dioxo-8-oxa-4,15-diazahexacyclo[14.7.1.02,14.04,13.06,11.020,24]tetracosa-1,6(11),12,14,16,18,20(24)-heptaen-23-yl]amino]-2-oxoethoxy]methylamino]-2-oxoethyl]-3-phenylpropanamide;hydrochloride
• InChI: InChI=1S/C42H45FN8O10.ClH/c1-3-42(59)26-12-31-38-24(17-51(31)40(57)25(26)18-61-41(42)58)37-28(10-9-23-21(2)27(43)13-29(50-38)36(23)37)48-35(55)19-60-20-47-33(53)15-46-39(56)30(11-22-7-5-4-6-8-22)49-34(54)16-45-32(52)14-44;/h4-8,12-13,28,30,59H,3,9-11,14-20,44H2,1-2H3,(H,45,52)(H,46,56)(H,47,53)(H,48,55)(H,49,54);1H/t28-,30-,42-;/m0./s1
• InChIKey: TVQVPAWTGTVHQV-SQLCOBTASA-N
• SMILES: CCC1(C2=C(COC1=O)C(=O)N3CC4=C5C(CCC6=C5C(=CC(=C6C)F)N=C4C3=C2)NC(=O)COCNC(=O)CNC(=O)C(CC7=CC=CC=C7)NC(=O)CNC(=O)CN)O.Cl

Gly-Gly-Phe-Gly-NH-O-CO-Exatecan hydrochloride (Cat No.: I040115) is a peptide–drug conjugate linker combining a short peptide sequence (Gly-Gly-Phe-Gly) with Exatecan, a potent topoisomerase I inhibitor. The peptide moiety serves as a cleavable linker, allowing for targeted drug release in the tumor microenvironment, typically in antibody-drug conjugate (ADC) strategies. Upon enzymatic cleavage, Exatecan is released to induce DNA damage and apoptosis in cancer cells. This conjugate is studied for its potential in targeted chemotherapy, improving specificity and reducing systemic toxicity in cancer treatment.

Reference

[1]. Joto N, et al. DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant. Int J Cancer. 1997;72(4):680-686.
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[2]. Thomas A, et al. Antibody-drug conjugates for cancer therapy. Lancet Oncol. 2016;17(6):e254-e262.
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