2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. Topoisomerase ADC Payload
  4. DXd

DXd  (Synonyms: Exatecan derivative for ADC)

Cat. No.: HY-13631D Purity: 99.30%
COA
SDS
Handling Instructions Technical Support

DXd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).

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

CAS No. : 1599440-33-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of DXd:

DXd Related Antibodies

Top Publications Citing Use of Products

    DXd purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 2;16(1):3167.  [Abstract]

    low cytometry assessment of surface CD47 expression on Au565 cells after 2 days of treatment with DXd (10-250 nM) or DM1.

    DXd purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 2;16(1):3167.  [Abstract]

    Various indicated cancer lines were seeded at low density and treated with titrated doses of DXd (1-10000 nM) or DM1, with DMSO solvent used as control treatment group. Cells were cultured for 5 days or until control groups reached >90% confluency. Cell viability and drug induced toxicity were assessed by cellular ATP quantification using using CellTiter-Glo Luminescent Cell Viability Assay following manufacturer’s protocol.

    DXd purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2023 Nov 1;29(21):4385-4398.  [Abstract]

    Apoptosis assay of DXd (100 nmol/L) in combination with adavosertib in MKN7 cells using Annexin V labeling.

    DXd purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2023 Nov 1;29(21):4385-4398.  [Abstract]

    Immunoblot of cyclin E, γH2AX, and pCHK1 in MKN7 cells following treatment with DXd (100 nmol/L) and T-DXd in combination with adavosertib for 24 or 96 hours. CCNE1, cyclin E1; DXd, deruxtecan; ERBB2, Erb-B2 receptor tyrosine kinase 2; T-DXd, trastuzumab deruxtecan.

    DXd purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2021 Mar 9;14(3):247.  [Abstract]

    Passive cell membrane diffusion of Exatecan and DXd payloads as assayed by a Corning® GentestTM PAMPA assay.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    DXd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).

    IC50 & Target[1]

    Topoisomerase I

    0.31 μM (IC50)

    Camptothecins

     

    In Vitro

    DXd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). DXd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s of 1.43 nM-4.07 nM, but the control IgG-ADC (DXd is the payload) shows no inhibition on the four cell lines (with HER2 expression). DS-8201a (DXd is the payload) displays significant suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines, with IC50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC50, >10,000 ng/mL)[1].

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

    DXd Related Antibodies
    In Vivo

    DS-8201a (DXd is the payload, 10 mg/kg, i.v.) shows potent antitumor activity in HER2-positive models with KPL4, JIMT-1, and Capan-1 and in HER2 low-expressing ST565 and ST313 models with HER2 IHC 1+/FISH-negative expression[1].

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

    493.48

    Formula

    C26H24FN3O6
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5NC(CO)=O)C(C)=C(F)C=C6N=C4C3=C2)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 40 mg/mL (81.06 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 2.0264 mL 10.1321 mL 20.2642 mL
    5 mM 0.4053 mL 2.0264 mL 4.0528 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.30%

    SDS (624 KB)

    COA (261 KB) HNMR (309 KB) RP-HPLC (95 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cells are seeded to a 96-well plate at 1,000 cells per well. After overnight incubation, Dxd is added. Cell viability is evaluated after 6 days using a CellTiter-Glo Luminescent Cell Viability Assay. For the detection of HER2 expression in each cell line, cells are incubated on ice for 30 minutes with FITC Mouse IgG1, κ Isotype Control, or anti-HER2/neu FITC. After washing, the labeled cells are analyzed by FACSCalibur. Relative mean fluorescence intensity (rMFI) is calculated[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Briefly, each cell suspension or tumor fragment is inoculated subcutaneously into specific pathogen-free female nude mice. When the tumor has grown to an appropriate volume, the tumor-bearing mice are randomized into treatment and control groups based on the tumor volumes, and dosing is initiated on day 0. Each substance (DS-8201a, 1 or 10 mg/kg, i.v.; Dxd is the payload) is administered intravenously to the mice. Tumor growth inhibition (TGI, %) is calculated[1].

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0264 mL 10.1321 mL 20.2642 mL 50.6606 mL
    5 mM 0.4053 mL 2.0264 mL 4.0528 mL 10.1321 mL
    10 mM 0.2026 mL 1.0132 mL 2.0264 mL 5.0661 mL
    15 mM 0.1351 mL 0.6755 mL 1.3509 mL 3.3774 mL
    20 mM 0.1013 mL 0.5066 mL 1.0132 mL 2.5330 mL
    25 mM 0.0811 mL 0.4053 mL 0.8106 mL 2.0264 mL
    30 mM 0.0675 mL 0.3377 mL 0.6755 mL 1.6887 mL
    40 mM 0.0507 mL 0.2533 mL 0.5066 mL 1.2665 mL
    50 mM 0.0405 mL 0.2026 mL 0.4053 mL 1.0132 mL
    60 mM 0.0338 mL 0.1689 mL 0.3377 mL 0.8443 mL
    80 mM 0.0253 mL 0.1267 mL 0.2533 mL 0.6333 mL
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    DXd 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:

    DXd1599440-33-1Exatecan derivative for ADCTopoisomeraseADC PayloadADC CytotoxinHER2-targetingADCInhibitorinhibitorinhibit

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