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Exatecan mesylate

Names

[ CAS No. ]:
197720-53-9

[ Name ]:
Exatecan mesylate

[Synonym ]:
DX-8951f
Exatecan mesylate (USAN)
UNII-D2VJ1CC26Q
Exatecan mesylate hydrate

Biological Activity

[Description]:

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[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase
Signaling Pathways >> Antibody-drug Conjugate >> ADC Cytotoxin

[Target]

Topoisomerase I:2.2 μM (IC50)


[References]

[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C24H22FN3O4S.CH4O3S.2H2O

[ Molecular Weight ]:
567.58

[ Exact Mass ]:
567.16900

[ PSA ]:
188.65000

[ LogP ]:
3.62960

[ Vapour Pressure ]:
2.47E-28mmHg at 25°C

Related Compounds