Exatecan
Based on 24 publication(s) in Google Scholar
Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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- Pureza: 99.96%
- No. CAS: 171335-80-1
- Fòrmula: C24H22FN3O4
- Peso molecular:435.45
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Exatecan
More- Nature. 2026 Jun 24.
- Nature. 2024 Apr;628(8007):416-423. [Abstract]
- Mol Cancer. 2025 Oct 13;24(1):253. [Abstract]
- Cancer Res. 2025 Oct 9. [Abstract]
- Acta Pharm Sin B. 2026 May 19.
- Acta Pharmacol Sin. 2025 Sep 10. [Abstract]
- Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]
- Pharmaceuticals (Basel). 2021 Mar 9;14(3):247. [Abstract]
- Mol Pharm. 2023 Jan 2;20(1):491-499. [Abstract]
- J Pharm Biomed Anal. 2025 Jun 15:258:116746. [Abstract]
- New J Chem. 2025 Jan 06.
- Cornell University. 2025.
- Patent. US20250295798A1.
- Patent. US20250242044A1.
- Cornell University. 2025.
- Patent. US20250161473A1.
- Patent. US20250161295A1.
- Patent. US20240374749A1.
- Research Square Preprint. 2024 Nov 06.
- Patent. US20240216525A1.
- Patent. US20240191272A1.
- Patent. US20240190973A1.
- Patent. US20220162323A1.
- Patent. US20210009719A1.
Customer Validation & Images
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WB
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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PK/PD Analysis
Ver todos los productos específicos de isoformas ADC Payloads
MoreVer todos los productos específicos de isoformas Topoisomerase
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Actividad biológica
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Camptothecins |
Exatecan is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI50s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively[1]. Exatecan Mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respctively. Exatecan Mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells[3].
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 171335-80-1
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Appearance Solid
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Peso molecular 435.45
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Fòrmula C24H22FN3O4
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Color Yellow to brown
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SMILES
O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5N)C(C)=C(F)C=C6N=C4C3=C2)=O
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Synonyms
DX-8951
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (24)
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Journal Impact Factor
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Most Recent
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Nature
2024 Apr;628(8007):416-423. PMID: 38538786 -
Mol Cancer
Harnessing ExDNA for precision exatecan delivery in cancer: a novel antibody-drug conjugate approach. [Abstract]2025 Oct 13;24(1):253. PMID: 41077566
Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2025 Oct 13;24(1):253. [Abstract]
Western blot analysis of B1-5V (BRCA1-) and B2-4V (BRCA2-) cells treated with PBS (NT, no treatment), V66-exatecan (100 nM) ADC for 1-24 h, or V66 alone (24 h). In samples treated with V66-exatecan ADC, a time-dependent accumulation of DNA damage is observed, as indicated by the increased γH2AX and pATM signals, along with a time-dependent down-regulation of TOP1.
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Cancer Res
2025 Oct 9. PMID: 41066595 -
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Acta Pharmacol Sin
HER3 upregulation reduces DS-8201 sensitivity in HER2-positive tumor cells by ATR/CHK1/FoxO1 signaling cascade. [Abstract]2025 Sep 10. PMID: 40931042 -
Mol Cancer Ther
AMT-562, a Novel HER3-targeting Antibody-Drug Conjugate, Demonstrates a Potential to Broaden Therapeutic Opportunities for HER3-expressing Tumors. [Abstract]2023 Sep 5;22(9):1013-1027. PMID: 37302522
Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]
In vivo efficacy of AMT-562, Ab562-T1000-Exatecan (10 mg/kg; i.v.), and P-GGFG-DXd in PC9 xenograft model.
Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]
In vitro cytotoxicity of Exatecan and DXd in HER3-expressing cells. Cells were incubated with a concentration series of Exatecan or DXd for 5 days. Cell viability was measured by CCK-8 and IC50 for each cell line was calculated from cell viability-concentration plot.
Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]
Representative hematoxylin and eosin staining of toxicity organs of AMT-562 and Ab562-T1000-Exatecan (ADC; 30 mg/kg; i.v.). Scale bar, 200 mm.
Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]
Single dose pharmacokinetic profiles of AMT-562 (ADC) and Ab562-GGFG-DXd in mice. ADCs were intravenously administered to mice at the dose of 10 mg/kg.
Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]
Patient-derived colon cancer organoids response to AMT-562 (ADC) and P-GGFG-DXd. Representative images of brightfield (left) and live/dead cells (right) for CO117 was shown. Colon cancer PDOs were treated with AMT-562 or P-GGFG-DXd at a serial concentration for 6 days. Live cells were stained by Calcein AM (green) and dead cells by PI (red).
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Pharmaceuticals (Basel)
Exatecan Antibody Drug Conjugates Based on a Hydrophilic Polysarcosine Drug-Linker Platform. [Abstract]2021 Mar 9;14(3):247. PMID: 33803327
Exatecan purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2021 Mar 9;14(3):247. [Abstract]
Tra-Exa-PSAR10 and Tra-Exa-PSAR0 (0.01-10 nM, 6 days). In vitro cytotoxicity of ADCs in breast and gastric HER2+ and HER2- (MCF-7) cancer cell lines after 6-day exposure to trastuzumab conjugates, as assayed by MTT assay, n = 3.
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Mol Pharm
Identification of 5-Carboxyfluorescein as a Probe Substrate of SLC46A3 and Its Application in a Fluorescence-Based In Vitro Assay Evaluating the Interaction with SLC46A3. [Abstract]2023 Jan 2;20(1):491-499. PMID: 36458938 -
J Pharm Biomed Anal
Development and optimization of a high-throughput LC-MS/MS method for the simultaneous determination of Exatecan and its Cathepsin B-sensitive prodrug, and ARV-825 in rat plasma: Application to pharmacokinetic study. [Abstract]2025 Jun 15:258:116746. PMID: 39955884 -
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Solvente y solubilidad
DMSO : 20 mg/mL (45.93 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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
sup>[3]Cells (5×106) are lysed with SDS buffer (10 mM HEPES, 2 mM orthovanadate, 10 mM NaF, 10 mM pyrophosphate, 1 mMPMSF, 10 µg/mL leupeptin, 10% 2-mercaptoethanol, 10% glycerol,8% SDS, 42 mM Tris-HCl, 0.002% bromophenol blue, pH 7.4). Protein in the whole cell lysates is separated in 7.5% polyacryl-amide gel and blotted onto nitrocellulose membrane. The membrane is treated with anti-Topo I human antibody and subsequently, with horseradish peroxidase-conjugated protein A. The Topo I-specific band is detected with ECL reagents. To obtain a nuclear extract, cells (5×107) are washed with ice-cold buffer (2 mM K2HPO4, 5 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 0.1 mM dithiothreitol), resuspended in buffer containing 0.35% Triton-X100 and PMSF and then incubated on ice for 10 min. The resulting lysates are centrifuged, and precipitates are then incubated with buffer containing 0.35 M NaCl for 1 hr at 4°C. After centrifugation (18,000g, 10 min), the protein concentration of the supernatant (nuclear extract) is determined by Bradford’s method using a protein assay kit. The same amount of nuclear protein is analyzed by Western blotting analysis using anti-Topo I antibody[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Growth inhibition experiments are carride out in 96-well flat-bottomed microplates, and the amount of viable cell at the end of the incubation is determined by MTT assay. Thus, 500-20000 cells/well in 150 μL of medium are plated and grown for 24 h (P388, CCRF-CEM and K562 cells for 4h), the drug (including Exatecan Mesylate, in 150 μL medium/well), or the medium alone as a control, is added, and the cells are cultured for an additional 3 days. After addition of MTT (20 μL/well, 5 mg/mL in phosphate-buffered saline), the plates are incubated for 4 h and centrifuged at 800 g for 5 min, then the medium is removed and the blue dye formed is dissolved in 150 μL of DMSO. the absorbance is measured at 540 nm using a Microplate Reader model 3550[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
At 3 weeks after BxPC-3-GFP and MIA-PaCa-2-GFP orthotopic implantation, mice are randomized into five different groups of 5 mice each for treatment purposes. Group 1 serves as the negative control and does not receive any treatment. Groups 2 and 3 are treated with Exatecan Mesylate at 25 and 15 mg/kg/dose, respectively. Groups 4 and 5 receive gemcitabine treatments at 300 and 150 mg/kg/dose, respectively. At 6 weeks after BxPC-3-GFP orthotopic implantation, mice are randomized into three different groups of 20 mice each for treatment purposes. Group 1 serves as the negative control and does not receive any treatment. Group 2 is treated with 25 mg/kg/dose Exatecan Mesylate and group 3 receives 300 mg/kg/dose gemcitabine. Dosing for both drugs is performed once a week for 3 weeks, discontinued for 2 weeks, and then continued for another 3 weeks. In both early and late cancer models, primary tumor size and body weights are measured once a week. Tumor volumes are calculated using the formula a × b2 × 0.5, where a and b represent the larger and smaller diameters, respectively. At the termination of the studies, mice are sacrificed and explored. Final tumor weights and direct GFP images of primary tumor and metastases are recorded for each mouse. The tumor growth IR is calculated using the formula IR (%) = (1 − TWt/TWc) × 100, where TWt and TWc are the mean tumor weight of treated and control groups, respectively[2].
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 (286 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Mitsui I, et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn J Cancer Res. 1995 Aug;86(8):776-82. [Content Brief]
[2]. Sun FX, et al. Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model. Cancer Res. 2003 Jan 1;63(1):80-5. [Content Brief]
[3]. Joto N, et al. DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant. Int J Cancer. 1997 Aug 7;72(4):680-6. [Content Brief]
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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 2.2965 mL | 11.4824 mL | 22.9647 mL | 57.4119 mL |
| 5 mM | 0.4593 mL | 2.2965 mL | 4.5929 mL | 11.4824 mL | |
| 10 mM | 0.2296 mL | 1.1482 mL | 2.2965 mL | 5.7412 mL | |
| 15 mM | 0.1531 mL | 0.7655 mL | 1.5310 mL | 3.8275 mL | |
| 20 mM | 0.1148 mL | 0.5741 mL | 1.1482 mL | 2.8706 mL | |
| 25 mM | 0.0919 mL | 0.4593 mL | 0.9186 mL | 2.2965 mL | |
| 30 mM | 0.0765 mL | 0.3827 mL | 0.7655 mL | 1.9137 mL | |
| 40 mM | 0.0574 mL | 0.2871 mL | 0.5741 mL | 1.4353 mL |
Exatecan Related Classifications
HY-13631 Related Classifications
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