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MC-Val-Cit-PAB-vinblastine

  CAS No.: 2055896-92-7   Cat No.: BADC-00857   Purity: >98.0% 4.5  

MC-Val-Cit-PAB-vinblastine is a drug-linker conjugate for ADC with potent antitumor activity by using vinblastine (an microtubule protein inhibitor), linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-vinblastine

Structure of 2055896-92-7

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Category
ADC Cytotoxin
Molecular Formula
C74H97N10O15
Molecular Weight
1366.62
Shipping
Room temperature, or blue ice upon request.
Shipping
Store at -20 °C, keep in dry and avoid sunlight.

* For research and manufacturing use only. We do not sell to patients.

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IUPAC Name
methyl (1R,9R,10S,11R,12R,19R)-11-acetyloxy-4-[(1R,13S,15R,17S)-1-[[4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrol-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl]-17-ethyl-17-hydroxy-13-methoxycarbonyl-11-aza-1-azoniatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraen-13-yl]-12-ethyl-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene-10-carboxylate
Canonical SMILES
CCC1(CC2CC(C3=C(CC[N+](C2)(C1)CC4=CC=C(C=C4)NC(=O)C(CCCNC(=O)N)NC(=O)C(C(C)C)NC(=O)CCCCCN5C(=O)C=CC5=O)C6=CC=CC=C6N3)(C7=C(C=C8C(=C7)C91CCN2C9C(C=CC2)(C(C(C1N8C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O
InChI
InChI=1S/C74H96N10O15/c1-10-70(94)39-47-40-73(67(91)97-8,52-37-51-55(38-56(52)96-7)81(6)65-72(51)31-35-82-33-18-30-71(11-2,64(72)82)66(99-45(5)85)74(65,95)68(92)98-9)61-50(49-19-14-15-20-53(49)78-61)29-36-84(42-47,43-70)41-46-23-25-48(26-24-46)77-62(89)54(21-17-32-76-69(75)93)79-63(90)60(44(3)4)80-57(86)22-13-12-16-34-83-58(87)27-28-59(83)88/h14-15,18-20,23-28,30,37-38,44,47,54,60,64-66,78,94-95H,10-13,16-17,21-22,29,31-36,39-43H2,1-9H3,(H5-,75,76,77,79,80,86,89,90,93)/p+1/t47-,54-,60-,64-,65+,66+,70-,71+,72+,73-,74-,84-/m0/s1
Solubility
10 mm in DMSO
Appearance
Solid
Shelf Life
0-4°C for short term (days to weeks), or -20°C for long term (months).
Shipping
Room temperature, or blue ice upon request.
Storage
Store at -20 °C, keep in dry and avoid sunlight.
Form
Solid

MC-Val-Cit-PAB-vinblastine is a potent peptide-drug conjugate (PDC) that combines the cytotoxicity of vinblastine with the targeted delivery capabilities of a peptide sequence. One key application is in targeted cancer therapy. The conjugate leverages the specificity of the Val-Cit linker to selectively release vinblastine within cancer cells. This targeted approach minimizes systemic toxicity, enhancing the therapeutic index by ensuring the drug is predominantly active in the tumor site, where it can efficiently inhibit cancer cell division.

Another prominent application of MC-Val-Cit-PAB-vinblastine is in the field of drug delivery systems. The conjugate's design allows for the controlled release of vinblastine through enzymatic cleavage at the Val-Cit junction, which is highly sensitive to the activity of cancer-specific proteases. This ensures that the drug is only activated within the tumor microenvironment, offering a mechanism for overcoming the challenges of traditional chemotherapy, such as off-target effects and poor drug bioavailability.

MC-Val-Cit-PAB-vinblastine also plays a crucial role in improving the efficacy of combination therapies. When used alongside other therapeutic agents, it can enhance the overall treatment outcome by providing synergistic effects. For instance, combining this PDC with immune checkpoint inhibitors or other cytotoxic agents can create a multi-pronged attack on the tumor, increasing the likelihood of a sustained therapeutic response. The ability to fine-tune the drug release via the peptide linker further augments this synergism.

Lastly, MC-Val-Cit-PAB-vinblastine is a promising candidate for preclinical and clinical research in personalized medicine. The conjugate can be engineered with different peptides to target specific tumor markers, making it highly adaptable for a wide range of cancers. This customization enables more precise and effective treatment regimens tailored to individual patient profiles, which is essential for improving patient outcomes in precision oncology.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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