mDPR-Val-Cit-PAB-MMAE consists the ADCs linker (mDPR-Val-Cit-PAB) and potent tubulin inhibitor (MMAE), mDPR-Val-Cit-PAB-MMAE is an antibody drug conjugate.
CAT No: R1901
CAS No:1491152-26-1
Synonyms/Alias:mDPR-Val-Cit-PAB-MMAE;1491152-26-1;SCHEMBL17254422;CS-5430;DA-65306;HY-19813;G70025;
Chemical Name:N-[(2S)-3-Amino-2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanoyl]-L-valyl-N-{4-[(5S,8S,11S,12R)-11-[(2S)-2-butanyl]-12-(2-{(2S)-2-[(1R,2R)-3-{[(1S,2R)-1-hydroxy-1-phenyl-2-propanyl]amino}-1-methoxy-2 ;-methyl-3-oxopropyl]-1-pyrrolidinyl}-2-oxoethyl)-5,8-diisopropyl-4,10-dimethyl-3,6,9-trioxo-2,13-dioxa-4,7,10-triazatetradec-1-yl]phenyl}-N5-carbamoyl-L-ornithinamide
mDPR-Val-Cit-PAB-MMAE is a synthetic peptide-drug conjugate (PDC) that combines a peptide linker sequence with a potent cytotoxic agent, monomethyl auristatin E (MMAE), through a valine-citrulline (Val-Cit) dipeptide and a para-aminobenzyl (PAB) self-immolative spacer. The design of this molecule is grounded in advanced peptide chemistry and targeted drug delivery research, where the stability and enzymatic cleavability of the Val-Cit linker are crucial for controlled payload release. With its modular structure, mDPR-Val-Cit-PAB-MMAE serves as a valuable model system for investigating site-specific conjugation strategies, linker stability, and the development of next-generation antibody-drug conjugates (ADCs) or related targeted therapeutics in a research setting.
Conjugation strategy optimization: The peptide-based linker in mDPR-Val-Cit-PAB-MMAE is widely studied for its role in facilitating the stable attachment of cytotoxic payloads to targeting moieties such as antibodies or peptides. Researchers utilize this compound to evaluate conjugation chemistries, linker stability under physiological conditions, and the efficiency of payload release upon exposure to specific intracellular enzymes, such as cathepsin B. Such studies help optimize linker design parameters to achieve maximal payload delivery while minimizing premature release, thereby informing the rational development of more effective and selective conjugates.
Enzymatic cleavage mechanism studies: The Val-Cit dipeptide linker is a well-characterized substrate for lysosomal proteases, particularly cathepsin B, making mDPR-Val-Cit-PAB-MMAE a preferred model for mechanistic studies of enzyme-triggered drug release. By employing this compound in cell-free systems or cellular models, researchers can elucidate the kinetics and specificity of proteolytic cleavage, assess the stability of the linker in plasma versus lysosomal environments, and compare alternative dipeptide sequences for improved selectivity. These insights directly impact the design of peptide linkers for targeted delivery systems.
Payload release profiling: The PAB self-immolative spacer in the conjugate facilitates efficient release of MMAE upon enzymatic cleavage of the Val-Cit linker. Investigators leverage mDPR-Val-Cit-PAB-MMAE to study the dynamics of payload liberation, including intermediate formation, rate of self-immolation, and the quantification of free MMAE in various biological matrices. Such profiling is essential for understanding the pharmacokinetic and pharmacodynamic properties of peptide-drug conjugates and for optimizing linker-payload combinations for research applications.
Analytical method development: The structural complexity of mDPR-Val-Cit-PAB-MMAE makes it an excellent standard for the development and validation of analytical techniques, including HPLC, LC-MS, and bioanalytical assays. Laboratories employ this compound to calibrate detection methods for intact conjugates, monitor linker cleavage products, and quantify released payloads. The availability of a well-defined conjugate with a cleavable peptide linker and a potent cytotoxin supports robust analytical workflows crucial for quality control and in vitro characterization of experimental drug conjugates.
ADC and PDC research tool: mDPR-Val-Cit-PAB-MMAE is frequently utilized as a research tool in the field of antibody-drug conjugates and peptide-drug conjugates, where its modular design allows for systematic evaluation of linker-payload behavior. Scientists use it to benchmark new linker technologies, assess cytotoxic payload potency, and model the impact of linker modifications on conjugate efficacy. Its relevance extends to comparative studies of new conjugation platforms, supporting the iterative optimization of targeted delivery strategies in preclinical research environments.
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More