1. Cell Cycle/DNA Damage Cytoskeleton Antibody-drug Conjugate/ADC Related
  2. Microtubule/Tubulin ADC Cytotoxin
  3. Mertansine

Mertansine  (Synonyms: DM1; Maytansinoid DM1)

Cat. No.: HY-19792 Purity: 99.55%
COA Handling Instructions

Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).

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

Mertansine Chemical Structure

Mertansine Chemical Structure

CAS No. : 139504-50-0

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Customer Review

Based on 21 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Mertansine purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022: 121913.

    Free Mertansine (DM1; 20 nM; 24 h) is able to induce apoptosis in NCI-H929 cells.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC)[1][2].

    IC50 & Target

    Maytansinoids

     

    In Vitro

    Mertansine is a strong antiproliferative chemotherapeutics toward over 60 types of cancer cell lines[3].
    Mertansine (0-1 μg/mL) shows antitumor activity in malignant B16F10 melanoma cells, and inhibits tumor cell growth by inhibiting mitosis when combined with DTX[3].

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

    Cell Proliferation Assay

    Cell Line: Malignant B16F10 melanoma cells[3]
    Concentration: 0, 0.01, 0.1, and 1 μg/mL
    Incubation Time: 4 h
    Result: Showed antitumor activity in malignant B16F10 melanoma cells, with an IC50 of 0.092 μg/mL. Co-delivery of DTX and DM1, both of which inhibit tumor cell growth by inhibiting mitosis, is an effective strategy to achieve a combinatorial anticancer effect.
    In Vivo

    Mertansine (DM1) has a low maximum-tolerated dose (MTD) of 1 mg/kg[3]

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

    Clinical Trial
    Molecular Weight

    738.29

    Formula

    C35H48ClN3O10S

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    C[C@]1([C@@](CC(N(C(C=C2C=C3OC)=C3Cl)C)=O)([H])OC([C@H](C)N(C)C(CCS)=O)=O)[C@H]([C@@H]([C@](OC4=O)([H])C[C@]([C@](/C=C/C=C(C)/C2)([H])OC)(N4)O)C)O1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (84.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3545 mL 6.7724 mL 13.5448 mL
    5 mM 0.2709 mL 1.3545 mL 2.7090 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: 2.17 mg/mL (2.94 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.17 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.08 mg/mL (2.82 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 99.80%

    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 1.3545 mL 6.7724 mL 13.5448 mL 33.8620 mL
    5 mM 0.2709 mL 1.3545 mL 2.7090 mL 6.7724 mL
    10 mM 0.1354 mL 0.6772 mL 1.3545 mL 3.3862 mL
    15 mM 0.0903 mL 0.4515 mL 0.9030 mL 2.2575 mL
    20 mM 0.0677 mL 0.3386 mL 0.6772 mL 1.6931 mL
    25 mM 0.0542 mL 0.2709 mL 0.5418 mL 1.3545 mL
    30 mM 0.0451 mL 0.2257 mL 0.4515 mL 1.1287 mL
    40 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.8466 mL
    50 mM 0.0271 mL 0.1354 mL 0.2709 mL 0.6772 mL
    60 mM 0.0226 mL 0.1129 mL 0.2257 mL 0.5644 mL
    80 mM 0.0169 mL 0.0847 mL 0.1693 mL 0.4233 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:
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    Cat. No.:
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