SN 38

Biological Activity

SN 38 is an active metabolite of CPT-11 (Cat. No. 2688) that inhibits DNA topoisomerase I (IC₅₀ values are 0.74 and 1.9 μM in P388 and Ehrlich cells respectively). Inhibits DNA and RNA synthesis (IC₅₀ values are 0.077 and 1.3 μM respectively) but does not affect protein synthesis. Displays potent antitumor activity against a range of human tumor cell lines (IC₅₀ values are 3.3, 13, 19 and 22 nM for HCT-116, BEL-7402, HL60 and HELA cells respectively).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Regulation of senescence escape by the cdk4-EZH2-AP2M1 pathway in response to chemotherapy
   M Le Duff, J Gouju, B Jonchère, J Guillon, B Toutain, A Boissard, C Henry, C Guette, E Lelièvre, O Coqueret
   Cell Death Dis, 2018;9(2):199.
2. Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11.
   Kawato et al.
   Cancer Res., 1991;51:4187
3. Synthesis and antitumor activity of the hexacyclic camptothecin derivatives.
   Gao et al.
   Bioorg.Med.Chem.Lett., 2005;15:3233
4. Novel SN-38-incorporating ploymeric micelles, NK012, eradicate vascular endothelial growth factor-Secr.g bulky tumors.
   Koizumi et al.
   Cancer Res., 2006;66:10048

Product Datasheets