Exatecan mesylate dihydrate
Based on 24 publication(s) in Google Scholar
Exatecan (DX-8951) mesylate dihydrate 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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- CAS No.: 197720-53-9
- Formule: C24H22FN3O4S.CH4O3S.2H2O
- Masse moléculaire:567.58
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Exatecan mesylate dihydrate
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.
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Activité biologique
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Camptothecins |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
0.914 ng/mL
Compound: 42; DX-8951f
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Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
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[PMID: 38421819] |
| HCT-116 | GI50 |
0.347 ng/mL
Compound: 42; DX-8951f
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Growth inhibition of human HCT-116 cells incubated for 72 hrs by MTT assay
Growth inhibition of human HCT-116 cells incubated for 72 hrs by MTT assay
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[PMID: 38421819] |
| K562 | GI50 |
10.4 ng/mL
Compound: 42; DX-8951f
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Growth inhibition of human K562 cells incubated for 72 hrs by MTT assay
Growth inhibition of human K562 cells incubated for 72 hrs by MTT assay
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[PMID: 38421819] |
| MCF7 | GI50 |
0.322 ng/mL
Compound: 42; DX-8951f
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Growth inhibition of human MCF7 cells incubated for 72 hrs by MTT assay
Growth inhibition of human MCF7 cells incubated for 72 hrs by MTT assay
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[PMID: 38421819] |
Chemical Information
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CAS No. 197720-53-9
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Masse moléculaire 567.58
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Formule C24H22FN3O4S.CH4O3S.2H2O
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SMILES
CS(=O)(O)=O.N[C@@H]1C2=C3C(C(N4C3)=CC([C@](O)(C(OC5)=O)CC)=C5C4=O)=NC6=CC(F)=C(C)C(CC1)=C62.O.O
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Synonyms
DX-8951 mesylate dihydrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
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 mesylate dihydrate 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 mesylate dihydrate 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 mesylate dihydrate 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 mesylate dihydrate 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 mesylate dihydrate 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 mesylate dihydrate 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 mesylate dihydrate 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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Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Exatecan mesylate dihydrate Related Classifications
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