2. Antibody-drug Conjugate/ADC Related
  3. Drug-Linker Conjugates for ADC
  4. Deruxtecan

Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.

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

Deruxtecan Chemical Structure

Deruxtecan Chemical Structure

CAS No. : 1599440-13-7

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Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of Deruxtecan:

Deruxtecan Related Antibodies

Top Publications Citing Use of Products

    Deruxtecan purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2023 Jun 6;CCR-23-0103.  [Abstract]

    Immunoblot of cyclin E, γH2AX, and pCHK1 in MKN7 cells following treatment with DXd and T-DXd in combination with adavosertib for 24 or 96 hours. CCNE1, cyclin E1; DXd, deruxtecan (10 nM- 24-96 h); ERBB2, Erb-B2 receptor tyrosine kinase 2; T-DXd, trastuzumab deruxtecan.

    View All Drug-Linker Conjugates for ADC Isoform Specific Products:

    View All Isoforms
    Auristatin Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.

    IC50 & Target

    Camptothecins

     

    In Vitro

    Antibody-drug conjugates deliver anticancer agents selectively and efficiently to tumor tissue and have significant antitumor efficacy with a wide therapeutic window[2].

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

    Deruxtecan Related Antibodies
    Clinical Trial
    Molecular Weight

    1034.05

    Formula

    C52H56FN9O13
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(C=CC1=O)N1CCCCCC(NCC(NCC(N[C@@H](CC2=CC=CC=C2)C(NCC(NCOCC(N[C@@H]3C4=C5C(C(N6C5)=CC([C@](O)(C(OC7)=O)CC)=C7C6=O)=NC8=CC(F)=C(C)C(CC3)=C48)=O)=O)=O)=O)=O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, protect from light, stored under nitrogen

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

    Solvent & Solubility
    In Vitro: 

    DMF : 100 mg/mL (96.71 mM; Need ultrasonic)

    DMSO : 73.33 mg/mL (70.92 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 0.9671 mL 4.8354 mL 9.6707 mL
    5 mM 0.1934 mL 0.9671 mL 1.9341 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 1.75 mg/mL (1.69 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.75 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 (17.5 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.
    • Protocol 2

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

      Solubility: 1.75 mg/mL (1.69 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.75 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 (17.5 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.
    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: 99.94%

    SDS (393 KB)

    COA (0 KB) HNMR (0 KB) RP-HPLC (196 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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 / DMF 1 mM 0.9671 mL 4.8354 mL 9.6707 mL 24.1768 mL
    5 mM 0.1934 mL 0.9671 mL 1.9341 mL 4.8354 mL
    10 mM 0.0967 mL 0.4835 mL 0.9671 mL 2.4177 mL
    15 mM 0.0645 mL 0.3224 mL 0.6447 mL 1.6118 mL
    20 mM 0.0484 mL 0.2418 mL 0.4835 mL 1.2088 mL
    25 mM 0.0387 mL 0.1934 mL 0.3868 mL 0.9671 mL
    30 mM 0.0322 mL 0.1612 mL 0.3224 mL 0.8059 mL
    40 mM 0.0242 mL 0.1209 mL 0.2418 mL 0.6044 mL
    50 mM 0.0193 mL 0.0967 mL 0.1934 mL 0.4835 mL
    60 mM 0.0161 mL 0.0806 mL 0.1612 mL 0.4029 mL
    DMF 80 mM 0.0121 mL 0.0604 mL 0.1209 mL 0.3022 mL
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    Deruxtecan Related Classifications

    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.

    Keywords:

    Deruxtecan1599440-13-7MC-GGFG-DXDDrug-Linker Conjugates for ADCInhibitorinhibitorinhibit

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