Datopotamab deruxtecan (solution)
Based on 2 publication(s) in Google Scholar
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.
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- 純度: 99.98%
- CAS 番号: 2238831-60-0
- 分子量:149000 (average)
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保管条件:
-80°C, protect from light
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生物活性
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Topoisomerase I |
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.
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Cell Line:BxPC-3 human pancreatic cancer cells
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Concentration:10 μg/mL
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Incubation Time:15 min; 30 min; 1 h; 3 h
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Result:Internalized time-dependently.
Aggregated in perinuclear regions.
Partly colocalized with the lysosomal marker LAMP-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.
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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]
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Dosage:10 mg/kg
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Administration:i.v.; single dose
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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.
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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]
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Dosage:10 mg/kg
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Administration:i.v.; single dose
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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.
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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]
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Dosage:10 mg/kg
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Administration:i.v.; single dose
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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.
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Animal Model:Crl:CD(SD) (male and female, healthy)[2]
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Dosage:20 mg/kg; 60 mg/kg; 200 mg/kg
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Administration:i.v.; once every 3 weeks; 3 months
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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.
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Animal Model:(male and female, healthy)[2]
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Dosage:10 mg/kg; 30 mg/kg; 80 mg/kg
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Administration:i.v.; once every 3 weeks; 3 months
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2238831-60-0
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性状 Liquid
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分子量 149000 (average)
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Color Colorless to light yellow
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SMILES
[Datopotamab deruxtecan (solution)]
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別名
DS-1062 (solution); Dato-DXd (solution)
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輸送条件
Shipping with dry ice.
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保管条件
-80°C, protect from light
Publications (2)
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Journal Impact Factor
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Most Recent
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Anal Chem
Preclinical Evaluation of a Trop2-Targeted Peptide Probe for PET Imaging of Triple-Negative Breast Cancer. [Abstract]2025 Oct 28;97(42):23598-23608. PMID: 41105928
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.
純度とドキュメンテーション
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参考文献
[1]. Bardia A, et al. Datopotamab Deruxtecan in Advanced or Metastatic HR+/HER2- and Triple-Negative Breast Cancer: Results From the Phase I TROPION-PanTumor01 Study. J Clin Oncol. 2024;42(19):2281-2294. [Content Brief]
[2]. Okajima D, et al. Datopotamab Deruxtecan, a Novel TROP2-directed Antibody-drug Conjugate, Demonstrates Potent Antitumor Activity by Efficient Drug Delivery to Tumor Cells. Mol Cancer Ther. 2021;20(12):2329-2340. [Content Brief]
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Datopotamab deruxtecan (solution) 関連分類
HY-141598 関連分類
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