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Exatecan (mesylate)

Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL) . Exatecan mesylate can be used in cancer research.

Product Specifications

CAS Number

[169869-90-3]

Product Name Alternative

DX8951f

UNSPSC

12352005

Hazard Statement

H300, H340, H360

Target

ADC Payload; Topoisomerase

Type

Reference compound

Related Pathways

Antibody-drug Conjugate/ADC Related; Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Exatecan-Mesylate.html

Purity

99.98

Solubility

DMSO : 7.41 mg/mL (ultrasonic) |H2O : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=S(C)(O)=O.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

Molecular Formula

C25H26FN3O7S

Molecular Weight

531.55

Precautions

H300, H340, H360

References & Citations

[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.|[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.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture and light)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

Camptothecins

Citation 01

BioRxiv. 2025 April 25.|J Pharm Biomed Anal. 2025 Jun 15:258:116746.|Mol Cancer. 2025 Oct 13;24 (1) :253.|Mol Pharm. 2023 Jan 2;20 (1) :491-499.|Nature. 2024 Apr;628 (8007) :416-423.|New J Chem. 2025 Jan 06.|Patent. US20210009719A1.|Patent. US20220162323A1.|Patent. US20240190973A1.|Patent. US20240216525A1.|Patent. US20240374749A1.|Patent. US20250161295A1.|Patent. US20250161473A1.|Patent. US20250242044A1.|Patent. US20250295798A1.|Pharmaceuticals (Basel) . 2021 Mar 9;14 (3) :247.| Cornell University. 2025.|Acta Pharmacol Sin. 2025 Sep 10.|Cancer Res. 2025 Oct 9.|Mol Cancer Ther. 2023 Sep 5;22 (9) :1013-1027.|Patent. US20240191272A1.|Research Square Preprint. 2024 Nov 06.

Available Sizes

Curated Selection

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