MPMS-VA
MPMS-VA is a highly hydrophilic peptide cleavable linker that can be used for the construction of ADCs. MPMS-VA can be cleaved at the Val-Ala site by lysosomal cathepsin B in tumor cells. MPMS-VA can enhance the hydrophilicity of the antibody-drug conjugate linker-payload system. MPMS-VA improves the plasma stability of relevant ADCs and reduces the systemic release of free payload. MPMS-VA can be applied in research related to solid tumors with co-expression of EGFR/HER2, such as lung cancer, breast cancer, gastric cancer, and urothelial carcinoma.
For research use only. We do not sell to patients.
- Formula: C39H65N5O16S
- Molecular Weight:892.02
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
MPMS-VA, a highly hydrophilic peptide-based cleavable linker for GenSci139, preserves the integrity of the conjugated ADC and the homogeneous DAR distribution in plasma in vitro, and is specifically cleaved by lysosomal cathepsin B in tumor cells to release the topoisomerase I inhibitor payload GSC5181[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Molecular Weight 892.02
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Formula C39H65N5O16S
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SMILES
OC([C@H](C)NC([C@H](C(C)C)NC(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(CCCC#CC1=CN=C(S(=O)(C)=O)N=C1OC)=O)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)