Exatecan

• Description:

  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.

• Product Name Alternative:

  DX-8951

• 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.html

• Purity:

  99.93

• Solubility:

  DMSO : 20 mg/mL (ultrasonic)

• 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

• Molecular Formula:

  C24H22FN3O4

• Molecular Weight:

  435.45

• 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:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, sealed storage, away from moisture)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 3

• Isoform:

  Camptothecins

• Citation 01:

  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.|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.

• CAS Number:

  [171335-80-1]