CAS No.: 644981-35-1
Purity: ≥98%
HPLC
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Val-Cit-PAB-MMAE, a tubulin polymerase inhibitor, is a drug-linker conjugate for ADC. It contains an ADC linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE.
Structure of 644981-35-1
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| Size | Price | Stock | Quantity |
|---|---|---|---|
| 100 mg | $999 | In stock |
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Val-Cit-PAB-MMAE is a potent ADC Cytotoxin with Linker widely utilized in the development of targeted cancer therapeutics and antibody-drug conjugates (ADCs). This highly cytotoxic ADC Cytotoxin combines monomethyl auristatin E (MMAE) with a cleavable Val-Cit-PAB ADC Linker, providing precise delivery of the ADC payload to tumor cells. The linker design ensures stability during systemic circulation while enabling efficient intracellular release, which is critical for maintaining therapeutic efficacy and minimizing off-target toxicity. As a key component in ADC research, Val-Cit-PAB-MMAE facilitates the creation of next-generation bioconjugates for preclinical and translational oncology studies.
The mechanism of Val-Cit-PAB-MMAE relies on the antibody’s selective binding to tumor-associated antigens, followed by internalization into target cells. Once inside, lysosomal proteases cleave the Val-Cit-PAB linker, releasing the MMAE payload to disrupt microtubule dynamics, ultimately inducing apoptosis in malignant cells. This selective cytotoxic action underscores the importance of the ADC payload-linker combination in enhancing therapeutic precision. Researchers leverage Val-Cit-PAB-MMAE for evaluating ADC efficacy, cytotoxicity profiles, and linker stability, making it an essential tool in the design of targeted oncology treatments and advanced ADC platforms.
Val-Cit-PAB-MMAE also supports efficient bioconjugation strategies, allowing stable attachment to a variety of monoclonal antibodies. The protease-sensitive linker improves payload release kinetics while reducing systemic exposure, addressing common challenges in ADC formulation and optimization. Its versatility in conjugation chemistry makes it a valuable reagent for researchers exploring novel ADC payloads, linker technologies, and tumor-targeting strategies. Integrating Val-Cit-PAB-MMAE into ADC pipelines enhances drug selectivity, improves therapeutic index, and accelerates preclinical development of innovative antibody therapeutics.
Applications of Val-Cit-PAB-MMAE include preclinical evaluation of antibody-drug conjugates, ADC linker stability studies, and targeted cytotoxicity assays. It is widely applied in research focusing on oncology therapeutics, bioconjugation chemistry, and translational cancer studies, providing a reliable platform for testing ADC performance. By incorporating Val-Cit-PAB-MMAE into development workflows, scientists can optimize ADC payload delivery, linker cleavage efficiency, and overall drug efficacy, facilitating the advancement of next-generation antibody-based therapies and expanding the potential of precision cancer treatment strategies.
| Catalog | Product Name | CAS | Inquiry |
|---|---|---|---|
| BADC-00019 | Fmoc-VC-PAB-MMAE | 1350456-56-2 | |
| BADC-00849 | Acetylene-linker-Val-Cit-PABC-MMAE | 1411977-95-1 | |
| BADC-01448 | mDPR-Val-Cit-PAB-MMAE | 1491152-26-1 | |
| BADC-00958 | Amino-PEG4-Val-Cit-PAB-MMAE | 1492056-71-9 | |
| BADC-01348 | Val-Cit-PAB-MMAE TFA salt | 1608127-32-7 | |
| BADC-01435 | N-Ac-Cys-MC-VC-PAB-MMAE | 1628933-80-1 | |
| BADC-01408 | DBM(C6)-VC-PAB-MMAE | 1644228-55-6 | |
| BADC-01459 | MC-betaglucuronide-MMAE-1 | 1703778-92-0 | |
| BADC-01638 | OH-Glu-Val-Cit-PAB-MMAE | 1895916-23-0 | |
| BADC-00855 | SuO-Glu-Val-Cit-PAB-MMAE | 1895916-24-1 |
What is Val-Cit-PAB-MMAE?
Val-Cit-PAB-MMAE is a widely used ADC linker-payload system. It features a cleavable dipeptide linker (Valine-Citrulline or Val-Cit), a self-immolative spacer (p-aminobenzyl alcohol or PAB), and a potent payload (Monomethyl auristatin E or MMAE). This combination is designed for controlled payload release at the tumor site.
25/1/2017
We are interested in how the Val-Cit dipeptide linker functions.
The Val-Cit dipeptide linker is the key to the system's controlled release mechanism. It is specifically designed to be recognized and cleaved by lysosomal proteases, such as cathepsin B, which are highly expressed inside cancer cells. After the ADC is internalized by the target cell, the linker is cleaved, initiating the release of the cytotoxic payload.
10/8/2018
Dear team, could you explain the role of the PAB spacer?
The PAB spacer, or p-aminobenzyl alcohol, is a self-immolative group. Once the Val-Cit dipeptide is cleaved by the lysosomal enzymes, the PAB spacer undergoes an intramolecular rearrangement. This reaction releases the active MMAE payload from the linker, allowing it to exert its cytotoxic effects within the cancer cell.
9/9/2016
May I ask what the mechanism of action of the MMAE payload is?
MMAE, or monomethyl auristatin E, is a highly potent synthetic antimitotic agent. It works by inhibiting tubulin polymerization, which disrupts the cell's cytoskeleton and prevents cell division. This action leads to G2/M cell cycle arrest and apoptosis, or programmed cell death, in the targeted cancer cells.
13/10/2021
Good afternoon! Could you please explain why Val-Cit-PAB-MMAE is a preferred system for ADCs?
This system is preferred due to its balanced properties. The cleavable linker ensures the payload is released specifically within the tumor cell environment, minimizing systemic toxicity. The highly potent MMAE payload provides effective killing of cancer cells. This combination has demonstrated its efficacy and safety in multiple clinical applications.
19/9/2018
— Dr. Kevin Wallace, Senior Scientist (USA)
Val-Cit-PAB-MMAE quality enabled precise payload release studies critical for our ADC development.
9/9/2016
— Dr. Emma Collins, ADC Researcher (UK)
We were impressed by the consistency of Val-Cit-PAB-MMAE batches across several conjugation runs.
19/9/2018
— Dr. Hans Bauer, Medicinal Chemist (Germany)
Delivery timing and QC documentation for Val-Cit-PAB-MMAE helped us meet stringent experimental deadlines.
13/10/2021
— Dr. Laura King, Biochemist (Canada)
Reliable Val-Cit-PAB-MMAE allowed multiple in vitro cytotoxicity assays without variation issues.
25/1/2017
— Dr. Richard Moore, Lead Scientist (USA)
Technical support on Val-Cit-PAB-MMAE conjugation strategies significantly improved workflow efficiency.
— Dr. Camille Bernard, Research Scientist (France)
Consistent high-purity Val-Cit-PAB-MMAE and professional advice ensured reproducible data.
10/8/2018
Val-Cit-PAB-MMAE
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Val-Cit-PAB-MMAE
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