2. Immunology/Inflammation Antibody-drug Conjugate/ADC Related Cell Cycle/DNA Damage
  3. TROP2 Antibody-Drug Conjugates (ADCs) Topoisomerase
  4. Datopotamab deruxtecan (solution)

Datopotamab deruxtecan (solution)  (Synonyms: DS-1062 (solution); Dato-DXd (solution))

Cat. No.: HY-141598 Purity: 99.98%
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Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer.

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

CAS No. : 2238831-60-0

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Based on 2 publication(s) in Google Scholar

Datopotamab deruxtecan (solution) Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Datopotamab deruxtecan (solution)

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IF
In Vivo Efficacy Study
In Vivo Imaging

    Datopotamab deruxtecan (solution) purchased from MedChemExpress. Usage Cited in: Anal Chem. 2025 Oct 28;97(42):23598-23608.  [Abstract]

    Western blotting analysis of the expression level of Trop2 in MDA-MB-468 cells treated with different concentrations of Dato-DXd (0-8 μg/mL; 48 h).

    Datopotamab deruxtecan (solution) purchased from MedChemExpress. Usage Cited in: Anal Chem. 2025 Oct 28;97(42):23598-23608.  [Abstract]

    Immunofluorescence analysis of Trop2 expression in MDA-MB-468 cells treated with different concentrations of Dato-DXd (0-8 μg/mL; 48 h).

    Datopotamab deruxtecan (solution) purchased from MedChemExpress. Usage Cited in: Anal Chem. 2025 Oct 28;97(42):23598-23608.  [Abstract]

    Time course of tumor volume of MDA-MB-468 tumor-bearing mice treated with PBS, SG (10 mg/kg, tail vein injection), and Dato-DXd (10 mg/kg, tail vein injection).

    Datopotamab deruxtecan (solution) purchased from MedChemExpress. Usage Cited in: Anal Chem. 2025 Oct 28;97(42):23598-23608.  [Abstract]

    MicroPET imaging of MDA-MB-468 tumor-bearing mice at different time postinjection of [68Ga]Ga-NOTA-PEG2-WP8 during PBS, SG (10 mg/kg, tail vein injection) and Dato-DXd (10 mg/kg, tail vein injection) treatment for 0, 9, and 18 days, respectively. White dotted line circles indicate the tumor locations.

    Datopotamab deruxtecan (solution) purchased from MedChemExpress. Usage Cited in: Anal Chem. 2025 Oct 28;97(42):23598-23608.  [Abstract]

    Time-activity curve of tumor uptake of [68Ga]Ga-NOTA-PEG2-WP8 in MDA-MB-468 xenografts during Dato-DXd (10 mg/kg, tail vein injection) treatment.

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    Description

    Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer[1][2].

    IC50 & Target[1]

    Topoisomerase I

     

    In Vitro

    Datopotamab deruxtecan solution binds specifically to human TROP2[2].
    Datopotamab deruxtecan solution binds with similar affinity to human and cynomolgus monkey TROP2, and does not bind to rat or mouse TROP2[2].
    Datopotamab deruxtecan (100 μg/mL; 21 days) solution is stable in human, cynomolgus monkey, rat, and mouse plasma, with minimal DXd release (1.4%-5.5%) after 21 days of incubation at 37°C[2].
    Datopotamab deruxtecan (0.32-1000 nmol/L; 6 days) solution potently inhibits the growth of TROP2-high human cancer cell lines (FaDu, BxPC-3, Caov-3, NCI-N87, CFPAC-1, HCC1806, COR-L23) with GI50 values of 0.48-7.8 nM, but does not inhibit TROP2-low cell lines (LK-2, Calu-6)[2].
    Datopotamab deruxtecan (10 μg/mL) solution efficiently internalizes into TROP2-expressing human cancer cell lines (BxPC-3, Caov-3, CFPAC-1, COR-L23, FaDu, HCC1806, NCI-N87) with an average internalization rate of 68.5% after 3 hours of incubation at 37°C[2].
    Datopotamab deruxtecan (100 nM; 24 h) solution releases DXd in amounts that correlate positively with cell-surface TROP2 expression levels after 24 hours of incubation with TROP2-expressing human cancer cell lines[2].
    Datopotamab deruxtecan (10 μg/mL; 15 min-3 h) solution internalizes time-dependently into BxPC-3 human pancreatic cancer cells, traffics to perinuclear regions, and colocalizes with the lysosomal marker LAMP-2[2].
    Datopotamab deruxtecan (6-72 h) solution time-dependently induces DNA damage (via phosphorylation of H2AX, KAP1, Chk1) and apoptosis (via cleavage of PARP and caspase-3) in NCI-N87 human gastric cancer cells[2].

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

    Datopotamab deruxtecan (solution) Related Antibodies

    Immunofluorescence[2]

    Cell Line: BxPC-3 human pancreatic cancer cells
    Concentration: 10 μg/mL
    Incubation Time: 15 min; 30 min; 1 h; 3 h
    Result: Internalized time-dependently.
    Aggregated in perinuclear regions.
    Partly colocalized with the lysosomal marker LAMP-2.
    In Vivo

    Datopotamab deruxtecan (10 mg/kg; i.v.; single dose) solution induces potent tumor growth inhibition (TGI = 96%) in TROP2-expressing NCI-N87 gastric cancer xenografts via DXd accumulation and DNA damage induction[2].
    Datopotamab deruxtecan (10 mg/kg; i.v.; single dose) solution induces potent tumor growth inhibition (TGI = 85-100%) in TROP2-high NSCLC cell line-derived xenografts, with no activity in TROP2-low models[2].
    Datopotamab deruxtecan (10 mg/kg; i.v.; single dose) solution induces potent tumor growth inhibition (TGI = 77-98%) in TROP2-high NSCLC patient-derived xenografts[2].
    Datopotamab deruxtecan (20-200 mg/kg; i.v.; once every 3 weeks for 3 months) solution is well tolerated in rats at doses up to 200 mg/kg with no life-threatening toxicity, and the STD10 is greater than 200 mg/kg[2].
    Datopotamab deruxtecan (10-80 mg/kg; i.v.; once every 3 weeks for 3 months) solution has an HNSTD of 10 mg/kg in cynomolgus monkeys, with severe pulmonary toxicity observed at doses ≥30 mg/kg[2].

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

    Animal Model: CAnN.Cg-Foxn1nu/CrlCrlj (female, athymic nude, subcutaneous inoculation of 1×107 NCI-N87 human gastric cancer cells to establish a gastric cancer xenograft model)[2]
    Dosage: 10 mg/kg
    Administration: i.v.; single dose
    Result: Induced significant tumor growth inhibition with a TGI of 96% (P < 0.001).
    Accumulated DXd in tumor tissue, with measurable concentrations detected up to day 21 post-administration.
    Observed time-dependent phosphorylation of the DNA damage marker γH2AX in tumors through day 7 post-administration.
    Caused no obvious body weight loss or unforeseen events.
    Animal Model: CAnN.Cg-Foxn1nu/CrlCrlj (female, athymic nude, subcutaneous inoculation of human NSCLC cell lines: 6×106 Calu-3 cells, 5×106 NCI-H2170 cells, 5×106 HCC827 cells, 1×106 LK-2 cells, 6×106 Calu-6 cells, 5×106 EBC-1 cells, to establish a lung cancer xenograft model)[2]
    Dosage: 10 mg/kg
    Administration: i.v.; single dose
    Result: Induced significant tumor growth inhibition in TROP2-high NSCLC models: Calu-3 (TROP2 H-score 145) with TGI of 85% (P < 0.001), NCI-H2170 (TROP2 H-score 115) with TGI of 95% (P < 0.001), HCC827 (TROP2 H-score 220) with TGI of 90% (P < 0.001), and EBC-1 (TROP2 H-score 133) with TGI of 100% (P < 0.001).
    Caused no tumor growth inhibition in TROP2-low models (LK-2, TROP2 H-score 20; Calu-6, TROP2 H-score 0).
    Caused no obvious body weight loss or unforeseen events.
    Animal Model: Hsd:Athymic Nude-Foxn1nu (female, athymic nude, subcutaneous inoculation of patient-derived tumor fragments from NSCLC patients to establish a lung cancer xenograft model)[2]
    Dosage: 10 mg/kg
    Administration: i.v.; single dose
    Result: Induced significant tumor growth inhibition in all TROP2-high NSCLC patient-derived xenograft models: CTG-0163 (TROP2 H-score 262) with TGI of 77% (P < 0.001), CTG-0838 (TROP2 H-score 163) with TGI of 98% (P < 0.001), and CTG-1014 (TROP2 H-score 252) with TGI of 95% (P < 0.001).
    Caused no obvious body weight loss or unforeseen events.
    Animal Model: Crl:CD(SD) (male and female, healthy)[2]
    Dosage: 20 mg/kg; 60 mg/kg; 200 mg/kg
    Administration: i.v.; once every 3 weeks; 3 months
    Result: Caused no deaths or life-threatening toxicities at any dose tested.
    Induced body weight decrease at ≥60 mg/kg.
    Caused decreased white blood cells, reticulocytes, neutrophils, lymphocytes, albumin, and increased urea nitrogen at 200 mg/kg.
    Induced target organ toxicities: thymus changes at ≥20 mg/kg; kidney, intestine, and incisor changes at ≥60 mg/kg; and lung, skin, bone marrow, spleen, reproductive organ changes at 200 mg/kg.
    Determined the severely toxic dose in 10% of animals (STD10) was >200 mg/kg.
    Animal Model: (male and female, healthy)[2]
    Dosage: 10 mg/kg; 30 mg/kg; 80 mg/kg
    Administration: i.v.; once every 3 weeks; 3 months
    Result: Caused no deaths at any dose tested.
    Induced severe pulmonary toxicity (cell infiltration, edema, fibrosis) at ≥30 mg/kg (1 animal at 30 mg/kg, 2 animals at 80 mg/kg).
    Induced body weight decrease at ≥30 mg/kg.
    Induced target organ toxicities: intestinal changes at ≥10 mg/kg; lung, cornea, skin, thymus, liver changes at ≥30 mg/kg; and kidney, joint cartilage changes at 80 mg/kg.
    Showed reversibility of skin and corneal lesions (except pigmentation) after treatment withdrawal.
    Determined the highest non-severely toxic dose (HNSTD) to be 10 mg/kg based on pulmonary findings.
    Clinical Trial
    Molecular Weight

    149000 (average)

    CAS No.
    Appearance

    Liquid

    Color

    Colorless to light yellow

    SMILES

    [Datopotamab deruxtecan (solution)]
    Shipping

    Shipping with dry ice.
    Storage

    -80°C, protect from light
    Purity & Documentation

    Purity: 99.98%

    SDS (251 KB)

    COA (231 KB) Others (93 KB) SEC-HPLC (92 KB)

    Handling Instructions (2659 KB)
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    Keywords:

    Datopotamab deruxtecan (solution)2238831-60-0DS-1062 (solution) Dato-DXd (solution)TROP2Antibody-Drug Conjugates (ADCs)TopoisomeraseEGP-1M1S1GA733-1Antibody-Drug ConjugatesBxPC-3cynomolgus monkeyNCI-N87non-small cell lung cancerFaDuHCC1806COR-L23Caov-3NSCLC PDX modelsInhibitorinhibitorinhibit

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