1. Antibody-drug Conjugate/ADC Related
  2. Drug-Linker Conjugates for ADC
  3. Val-Cit-PAB-MMAE

Val-Cit-PAB-MMAE est un conjugué de liaison médicamenteuse pour l'ADC. Val-Cit-PAB-MMAE contient le lieur ADC (peptide Val-Cit-PAB) et un inhibiteur puissant de la tubuline MMAE (HY-15162). MMAE est un inhibiteurpuissant mitotique en inhibant la polymérisation de la tubuline.

Val-Cit-PAB-MMAE is a agent-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.

For research use only. We do not sell to patients.

CAS No. : 644981-35-1

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Val-Cit-PAB-MMAE:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Val-Cit-PAB-MMAE

In Vivo Efficacy Study

    Val-Cit-PAB-MMAE purchased from MedChemExpress. Usage Cited in: Patent. US20210093733A1.

    The administration of Val-Cit-PAB-MMAE (OBI-998-TBR)-F (0.3 mg/kg; i.v.; once weekly for 4 weeks), Val-Cit-PAB-MMAE (OBI-998-TBR)-A and OBI-998-MCCA was associated with moderate and statistically significant anti-tumor activity compared to the vehicle control group over the course of the study.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Val-Cit-PAB-MMAE is a agent-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.

    IC50 & Target

    Auristatin

     

    In Vitro

    ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    1123.43

    Formula

    C58H94N10O12

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC[C@H](C)[C@@H]([C@@H](CC(N1[C@@H](CCC1)[C@@H]([C@@H](C)C(N[C@H](C)[C@@H](O)C2=CC=CC=C2)=O)OC)=O)OC)N(C([C@H](C(C)C)NC([C@H](C(C)C)N(C(OCC3=CC=C(NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)N)=O)=O)C=C3)=O)C)=O)=O)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, stored under nitrogen

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 110 mg/mL (97.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.8901 mL 4.4507 mL 8.9013 mL
    5 mM 0.1780 mL 0.8901 mL 1.7803 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5.5 mg/mL (4.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (4.45 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *The compound is unstable in solutions, freshly prepared is recommended.

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.98%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 0.8901 mL 4.4507 mL 8.9013 mL 22.2533 mL
    5 mM 0.1780 mL 0.8901 mL 1.7803 mL 4.4507 mL
    10 mM 0.0890 mL 0.4451 mL 0.8901 mL 2.2253 mL
    15 mM 0.0593 mL 0.2967 mL 0.5934 mL 1.4836 mL
    20 mM 0.0445 mL 0.2225 mL 0.4451 mL 1.1127 mL
    25 mM 0.0356 mL 0.1780 mL 0.3561 mL 0.8901 mL
    30 mM 0.0297 mL 0.1484 mL 0.2967 mL 0.7418 mL
    40 mM 0.0223 mL 0.1113 mL 0.2225 mL 0.5563 mL
    50 mM 0.0178 mL 0.0890 mL 0.1780 mL 0.4451 mL
    60 mM 0.0148 mL 0.0742 mL 0.1484 mL 0.3709 mL
    80 mM 0.0111 mL 0.0556 mL 0.1113 mL 0.2782 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Val-Cit-PAB-MMAE
    Cat. No.:
    HY-100374
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