CAS No.: 863971-17-9
Purity: ≥98%
MS
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MC-Val-Cit-PAB-MMAF is a well-established ADC cytotoxin with a valine-citrulline cleavable linker and MMAF payload, facilitating efficient and selective drug release in tumor cells. This ADC conjugate is widely applied in targeted cancer therapy research. Keywords: MMAF payload, cleavable linker, ADC design, targeted cytotoxicity.
Structure of 863971-17-9
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| Size | Price | Stock | Quantity |
|---|---|---|---|
| 1 mg | $299 | In stock |
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MC-Val-Cit-PAB-MMAF is a targeted drug conjugate that combines the potent cytotoxic agent monomethyl auristatin F (MMAF) with a peptide linker system. MMAF is a highly effective microtubule inhibitor that disrupts cell division by preventing microtubule polymerization, leading to cell cycle arrest and apoptosis in rapidly dividing cells, such as those found in cancer. The MC-Val-Cit-PAB linker ensures that MMAF is delivered specifically to tumor cells by incorporating tumor-targeting peptides, thereby enhancing the precision and efficacy of the drug while minimizing off-target effects and systemic toxicity.
One of the primary applications of MC-Val-Cit-PAB-MMAF is in the development of antibody-drug conjugates (ADCs) for targeted cancer therapy. The peptide linker enables the conjugation of MMAF to antibodies or other targeting molecules that recognize specific tumor antigens. This allows for the selective delivery of MMAF to cancer cells, where it can exert its cytotoxic effects. By targeting tumor cells specifically, this approach minimizes damage to healthy cells and enhances the therapeutic index, making it a promising strategy for treating cancers that are resistant to conventional therapies.
MC-Val-Cit-PAB-MMAF also addresses challenges associated with conventional chemotherapy, such as drug resistance and toxicity. Many cancers develop resistance to traditional treatments, including those targeting microtubules, through various mechanisms such as drug efflux or changes in the microtubule network. The targeted nature of MC-Val-Cit-PAB-MMAF helps overcome these resistance mechanisms by concentrating the cytotoxic agent directly at the tumor site. This approach can improve the therapeutic efficacy of MMAF, even in resistant cancer strains, offering a more potent treatment option for patients with limited alternatives.
In addition, the use of MC-Val-Cit-PAB-MMAF enhances the pharmacokinetics of MMAF, improving its solubility, stability, and bioavailability. MMAF, like many potent cytotoxic agents, suffers from poor water solubility and a short half-life in circulation, which limits its effectiveness. The incorporation of the MC-Val-Cit-PAB linker system improves the pharmacokinetic profile of MMAF, allowing for more controlled release and prolonged circulation time. This controlled delivery enhances the overall therapeutic outcome while reducing the likelihood of side effects associated with peak drug concentrations.
| Catalog | Product Name | CAS | Inquiry |
|---|---|---|---|
| BADC-01432 | Cys-MC-MMAF | 1160590-05-5 | |
| BADC-00592 | MC-Alkyl-Hydrazine Modified MMAF | 1404071-64-2 | |
| BADC-01455 | Modified MMAF-C5-COOH | 1404071-65-3 | |
| BADC-00594 | PEG4-aminooxy-MMAF | 1415246-35-3 | |
| BADC-00617 | MMAF sodium | 1799706-65-2 | |
| BADC-01460 | DBM-MMAF | 1810001-93-4 | |
| BADC-00863 | DBCO-PEG4-Val-Cit-PAB-MMAF | 2244602-23-9 | |
| BADC-00751 | DBCO-PEG4-MMAF | 2360411-65-8 | |
| 2413724-69-1 | (R)-N-((S)-(2-(Di(adamantan-1-yl)phosphino)phenyl)(phenyl)methyl)-N,2-dimethylpropane-2-sulfinamide | 2413724-69-1 | |
| 389868-12-6 | Ac-Glu-Glu-Val-Val-Ala-Cys-pNA | 389868-12-6 |
What is MC-Val-Cit-PAB-MMAF and what is its function?
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for ADCs. It consists of the potent tubulin inhibitor MMAF, a cleavable dipeptide linker (Val-Cit), and a self-immolative spacer (PAB), connected via a maleimidocaproyl (MC) group. Its function is to provide a highly potent cytotoxic agent that is released within target cells upon lysosomal processing.
12/3/2019
Could you kindly advise how the linker system in MC-Val-Cit-PAB-MMAF works?
The linker system is designed for selective intracellular cleavage. The Val-Cit dipeptide is a substrate for the lysosomal protease cathepsin B, which is highly expressed in tumor cells. Upon ADC internalization, this enzyme cleaves the linker, releasing the PAB-MMAF intermediate. The PAB group then self-immolates, liberating the active MMAF payload.
20/2/2019
Could you kindly explain the significance of the MMAF payload?
MMAF (monomethyl auristatin F) is a highly potent synthetic antimitotic agent. Unlike some other payloads, MMAF's structure prevents it from being a substrate for efflux pumps, which can lead to drug resistance. Its potent tubulin-disrupting activity makes it an effective cytotoxic agent for targeted cell killing.
12/9/2019
Could you kindly explain how MC-Val-Cit-PAB-MMAF enhances ADC selectivity?
The design of MC-Val-Cit-PAB-MMAF is a cornerstone of targeted therapy. The cleavable linker is stable in circulation, but its selective cleavage by an enzyme enriched in lysosomes (cathepsin B) ensures the payload is primarily released inside the targeted tumor cell. This minimizes off-target toxicity and improves the overall safety and efficacy of the ADC.
15/9/2022
Good afternoon! Can MC-Val-Cit-PAB-MMAF be found in clinically approved ADCs?
Linker-payloads based on the MC-Val-Cit-PAB-MMAF system are a well-established and clinically validated technology. This system has been successfully utilized in several approved ADCs, demonstrating its reliability and effectiveness in delivering potent payloads to cancer cells in a controlled manner.
22/11/2016
— Dr. Laura Bennett, Senior Scientist (USA)
MC-Val-Cit-PAB-MMAF arrived with outstanding purity, enabling precise ADC conjugation in our preclinical studies.
12/9/2019
— Dr. Michael Carter, ADC Chemist (UK)
The batch consistency of MC-Val-Cit-PAB-MMAF ensured reproducible cytotoxicity results.
22/11/2016
— Dr. Stefan Müller, Medicinal Chemist (Germany)
Fast delivery and thorough QC documentation of MC-Val-Cit-PAB-MMAF helped us meet tight project deadlines.
15/9/2022
— Dr. Emily White, Biochemist (Canada)
Technical guidance provided for MC-Val-Cit-PAB-MMAF improved our conjugation efficiency.
12/3/2019
— Dr. Robert Thompson, Lead Scientist (USA)
High-purity MC-Val-Cit-PAB-MMAF consistently supported multiple in vitro ADC experiments.
— Dr. Camille Laurent, Pharmacology Scientist (France)
Responsive support combined with MC-Val-Cit-PAB-MMAF quality accelerated our project timelines.
20/2/2019
MC-Val-Cit-PAB-MMAF
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MC-Val-Cit-PAB-MMAF
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