DXd
Based on 14 publication(s) in Google Scholar
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).
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- Pureza: 99.30%
- No. CAS: 1599440-33-1
- Fòrmula: C26H24FN3O6
- Peso molecular:493.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) DXd
More- Nat Commun. 2025 Apr 2;16(1):3167. [Abstract]
- Adv Sci (Weinh). 2025 Oct 24:e06552. [Abstract]
- Adv Sci (Weinh). 2025 Apr;12(16):e2415577. [Abstract]
- Clin Cancer Res. 2023 Nov 1;29(21):4385-4398. [Abstract]
- Cell Rep. 2023 Nov 28;42(12):113503. [Abstract]
- Anal Chim Acta. 2024 May 15:1303:342537. [Abstract]
- Pharmaceuticals (Basel). 2021 Mar 9;14(3):247. [Abstract]
- Int J Mol Sci. 2023 Dec 18;24(24):17631. [Abstract]
- Int J Mol Sci. 2023 Nov 7;24(22):16056. [Abstract]
- Am J Cancer Res. 2023 Jan 15;13(1):161-175. [Abstract]
- bioRxiv. 2025 March 25.
- Research Square Preprint. 2024 Nov 06.
- Patent. US20240293379A1.
- Patent. US20210009719A1.
Customer Validation & Images
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Flow Cytometry
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Ver todos los productos específicos de isoformas Topoisomerase
MoreVer todos los productos específicos de isoformas ADC Payloads
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Actividad biológica
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Topoisomerase I 0.31 μM (IC50) |
Camptothecins |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1599440-33-1
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Appearance Solid
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Peso molecular 493.48
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Fòrmula C26H24FN3O6
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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
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Synonyms
Exatecan derivative for ADC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Commun
Effective extracellular payload release and immunomodulatory interactions govern the therapeutic effect of trastuzumab deruxtecan (T-DXd). [Abstract]2025 Apr 2;16(1):3167. PMID: 40175391
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.
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Adv Sci (Weinh)
Interactions of Antibody Drug Conjugate Anti-Tubulin and Topoisomerase I Inhibitor Payloads with Radiotherapy to Potentiate Immunotherapy. [Abstract]2025 Oct 24:e06552. PMID: 41133986 -
Adv Sci (Weinh)
Reprogramming the Tumor Immune Microenvironment with ICAM-1-Targeted Antibody‒Drug Conjugates and B7-H3-CD3 Bispecific Antibodies. [Abstract]2025 Apr;12(16):e2415577. PMID: 39996528 -
Clin Cancer Res
Adavosertib Enhances Antitumor Activity of Trastuzumab Deruxtecan in HER2-Expressing Cancers. [Abstract]2023 Nov 1;29(21):4385-4398. PMID: 37279095
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.
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Cell Rep
Engineering CD276/B7-H3-targeted antibody-drug conjugates with enhanced cancer-eradicating capability. [Abstract]2023 Nov 28;42(12):113503. PMID: 38019654 -
Anal Chim Acta
Quantifying payloads of antibody‒drug conjugates using a postcolumn infused-internal standard strategy with LC‒MS. [Abstract]2024 May 15:1303:342537. PMID: 38609272 -
Pharmaceuticals (Basel)
Exatecan Antibody Drug Conjugates Based on a Hydrophilic Polysarcosine Drug-Linker Platform. [Abstract]2021 Mar 9;14(3):247. PMID: 33803327
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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Int J Mol Sci
Generation and Characterization of SORT1-Targeted Antibody-Drug Conjugate for the Treatment of SORT1-Positive Breast Tumor. [Abstract]2023 Dec 18;24(24):17631. PMID: 38139459 -
Int J Mol Sci
Generation of a Novel SORT1×HER2 Bispecific Antibody-Drug Conjugate Targeting HER2-Low-Expression Tumor. [Abstract]2023 Nov 7;24(22):16056. PMID: 38003245 -
Am J Cancer Res
Combined inhibition of PARP and ATR synergistically potentiates the antitumor activity of HER2-targeting antibody-drug conjugate in HER2-positive cancers. [Abstract]2023 Jan 15;13(1):161-175. PMID: 36777513 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (624 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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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