Name: AmPEG6C2-Aur0131
Brand: BOC Sciences
Rating: 5 (1 reviews)

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Synonyms

((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((S)-1-(1-Amino-3,6,9,12,15,18-hexaoxahenicosan-21-oyl)-2-methylpyrrolidine-2-carboxamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanoyl)-L-phenylalanine

IUPAC Name

(2S)-2-[[(2R,3R)-3-[(2S)-1-[(3R,4S,5S)-4-[[(2S)-2-[[(2S)-1-[3-[2-[2-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoyl]-2-methylpyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl]-3-methoxy-2-methylpropanoyl]amino]-3-phenylpropanoic acid

Canonical SMILES

NCCOCCOCCOCCOCCOCCOCCC(N1[C@@](C(N[C@@H](C(C)C)C(N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(N2[C@H]([C@H](OC)[C@@H](C)C(N[C@@H](CC3=CC=CC=C3)C(O)=O)=O)CCC2)=O)=O)=O)(C)CCC1)=O

InChI

InChI=1S/C54H92N6O15/c1-10-39(4)48(44(68-8)37-46(62)59-22-14-18-43(59)49(69-9)40(5)50(63)56-42(52(65)66)36-41-16-12-11-13-17-41)58(7)51(64)47(38(2)3)57-53(67)54(6)20-15-23-60(54)45(61)19-24-70-26-28-72-30-32-74-34-35-75-33-31-73-29-27-71-25-21-55/h11-13,16-17,38-40,42-44,47-49H,10,14-15,18-37,55H2,1-9H3,(H,56,63)(H,57,67)(H,65,66)/t39-,40+,42-,43-,44+,47-,48-,49+,54-/m0/s1

InChIKey

JKVBOSLOHJCKQR-NOWWAFAQSA-N

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AmPEG6C2-Aur0131, a specialized compound with diverse applications in biological research and medical fields, offers a myriad of possibilities.

Drug Delivery Systems: Harnessing the potential of AmPEG6C2-Aur0131, researchers can pioneer advanced drug delivery systems that optimize the targeting and efficiency of therapeutic agents. By conjugating drugs with this compound, solubility, stability, and bioavailability are vastly improved, resulting in streamlined drug delivery processes that minimize side effects while maximizing therapeutic impact.

Imaging and Diagnostics: Within the realm of medical imaging and diagnostics, AmPEG6C2-Aur0131 shines as a molecular probe of exceptional caliber. Its unique properties afford high specificity and sensitivity in detecting molecular targets, facilitating early disease diagnosis. For instance, in fluorescence imaging, this compound grants insights into biological processes at the cellular and molecular levels, offering a comprehensive view of intricate biological phenomena.

Bioconjugation Studies: AmPEG6C2-Aur0131 assumes a pivotal role in bioconjugation studies, acting as a vital linker molecule for attaching diverse biomolecules. This function is essential for crafting complex bioconjugates utilized in targeted therapies and diagnostic assays. By enabling precise and stable conjugation of antibodies, peptides, or proteins, this compound elevates the functionality and efficacy of bioconjugates.

Tissue Engineering: In the realm of tissue engineering, AmPEG6C2-Aur0131 emerges as a cornerstone for modifying biomaterials and scaffolds to enhance their biocompatibility and functionality. Through integration into biomaterials, this compound fosters improved cell attachment, proliferation, and differentiation, thereby promoting tissue regeneration. This application holds significant promise in advancing materials for regenerative medicine and tissue repair, showcasing the transformative power of AmPEG6C2-Aur0131 in the field of biomedicine.

1.Optimal design, anti-tumour efficacy and tolerability of anti-CXCR4 antibody drug conjugates

Costa MJ, et al.

Antibody-drug conjugates (ADCs) are promising therapies for haematological cancers. Historically, their therapeutic benefit is due to ADC targeting of lineage-restricted antigens. The C-X-C motif chemokine receptor 4 (CXCR4) is attractive for targeted therapy of haematological cancers, given its expression in multiple tumour types and role in cancer "homing" to bone marrow. However, CXCR4 is also expressed in haematopoietic cells and other normal tissues, raising safety challenges to the development of anti-CXCR4 ADCs for cancer treatment. Here, we designed the first anti-CXCR4 ADC with favourable therapeutic index, effective in xenografts of haematopoietic cancers resistant to standard of care and anti-CXCR4 antibodies. We screened multiple ADC configurations, by varying type of linker-payload, drug-to-antibody ratio (DAR), affinity and Fc format. The optimal ADC bears a non-cleavable linker, auristatin as payload at DAR = 4 and a low affinity antibody with effector-reduced Fc. Contrary to other drugs targeting CXCR4, anti-CXCR4 ADCs effectively eliminated cancer cells as monotherapy, while minimizing leucocytosis. The optimal ADC selectively eliminated CXCR4+ cancer cells in solid tumours, but showed limited toxicity to normal CXCR4+ tissues, sparing haematopoietic stem cells and progenitors. Our work provides proof-of-concept that through empirical ADC design, it is possible to target proteins with broad normal tissue expression.