Name: Mal-VC-PAB-ABAEP-Azonafide
Brand: BOC Sciences
Rating: 5 (1 reviews)

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IUPAC Name

[4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrol-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[4-[2-[4-[2-(10-methoxy-14,16-dioxo-15-azatetracyclo[7.7.1.02,7.013,17]heptadeca-1(17),2,4,6,8,10,12-heptaen-15-yl)ethyl]piperazin-1-yl]ethylcarbamoyl]phenyl]carbamate

Canonical SMILES

O=C(N1CCN2CCN(CCNC(C3=CC=C(NC(OCC4=CC=C(NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC(CCCCCN5C(C=CC5=O)=O)=O)=O)=O)C=C4)=O)C=C3)=O)CC2)C6=C7C(C(OC)=CC=C7C1=O)=CC8=CC=CC=C68

InChI

InChI=1S/C61H71N11O12/c1-38(2)54(68-49(73)13-5-4-8-28-71-50(74)24-25-51(71)75)57(78)67-47(12-9-26-64-60(62)81)56(77)65-42-18-14-39(15-19-42)37-84-61(82)66-43-20-16-40(17-21-43)55(76)63-27-29-69-30-32-70(33-31-69)34-35-72-58(79)45-22-23-48(83-3)46-36-41-10-6-7-11-44(41)53(52(45)46)59(72)80/h6-7,10-11,14-25,36,38,47,54H,4-5,8-9,12-13,26-35,37H2,1-3H3,(H,63,76)(H,65,77)(H,66,82)(H,67,78)(H,68,73)(H3,62,64,81)/t47-,54-/m0/s1

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Mal-VC-PAB-ABAEP-Azonafide is a conjugate with versatile applications in targeted cancer therapy. The maleimide (Mal) group allows for efficient conjugation to thiol-containing biomolecules like antibodies or peptides, enabling the creation of antibody-drug conjugates (ADCs). The VC (Val-Cit) linker provides a cleavable bond, allowing for controlled release of the cytotoxic agent, Azonafide, within the target cells. The incorporation of the PAB (para-amino benzoic acid) group aids in the stability of the conjugate, while the ABAEP (amino butyl amido ethyl pyrrolidine) spacer contributes to solubility and flexibility, enhancing the overall pharmacokinetics of the compound. This makes Mal-VC-PAB-ABAEP-Azonafide a promising candidate for targeted drug delivery in oncology.

A major application of Mal-VC-PAB-ABAEP-Azonafide is in the development of targeted chemotherapy agents. Azonafide, a potent DNA-intercalating agent, is conjugated to antibodies or peptides through the maleimide group. This targeted approach allows for the selective delivery of Azonafide to cancer cells, minimizing off-target effects and reducing systemic toxicity. The cleavable VC linker ensures that Azonafide is released once the conjugate enters the tumor cell, where it can then bind to DNA and induce cell death. This precise delivery mechanism is vital for enhancing the efficacy of cancer therapies while limiting the negative side effects typically associated with conventional chemotherapy.

In addition to its use in ADCs, Mal-VC-PAB-ABAEP-Azonafide can be applied in the design of peptide-drug conjugates (PDCs) for the treatment of specific cancers or other diseases. Peptides that bind selectively to cancer-specific biomarkers can be conjugated to Azonafide via the maleimide group, enabling targeted drug delivery. The ABAEP spacer improves the stability of the conjugate, while the VC linker facilitates controlled drug release in the tumor microenvironment. This application ensures that the therapeutic agent is only activated within cancer cells, reducing the potential for damage to healthy tissues.

Mal-VC-PAB-ABAEP-Azonafide can also be used in drug resistance research, as it offers a platform for studying how cancer cells respond to targeted chemotherapy. By using this conjugate in experimental models, researchers can assess the efficacy of different targeting strategies, evaluate potential drug resistance mechanisms, and explore new ways to overcome resistance in cancer therapy. The ability to modify the linker, payload, and targeting moiety provides flexibility in designing experiments that examine the molecular basis of chemotherapy resistance and help identify novel therapeutic approaches.

1.ROR1 ANTIBODY IMMUNOCONJUGATES

LANNUTTI, Brian, et al.

Cancer is the second leading cause of human death next to coronary artery disease.Receptor tyrosine kinases (RTKs) play a key role in oncogenic transformation, growth andmetastases. RTKs regulate cell differentiation, proliferation, migration, angiogenesis, andsurvival. The receptor tyrosine kinase-like orphan receptor 1 (ROR1) is an evolutionarilyconserved type I membrane protein that belongs to the ROR subfamily and has extracellulardomains that contain immunoglobulin (Ig)-like, Frizzled, and Kringle domains. ROR 1-deficientmice display a variety of phenotypic defects within the skeletal and urogenital systems, as wellas postnatal growth retardation. ROR1 is expressed during embryogenesis and by a variety ofdifferent cancers, but not by normal post-partum tissues, and can be considered an oncoembryonic surface antigen. Functional data suggest that ROR1 may function in non-canonicalWNT-signaling to promote the survival of malignant cells.