SN-38

Biological Activity

SN-38 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

Product Citations

• 

  BMC Biol. 2021 May 20;19(1):108.

  Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
  SN-38 purchased from AbMole

• 

  Nat Commun. 2019 Dec 20;10(1):5799.

  Novel approach reveals genomic landscapes of single-strand DNA breaks with nucleotide resolution in human cells.
  SN-38 purchased from AbMole

Customer Product Validations & Biological Datas

	Source	Customer experimental result (2018).
	Method	Cell viability assay
	Cell Lines	MDA-MB-231 cells
	Concentrations	32nM
	Incubation Time	4 days
	Results	MDA-MB-231 cells were treated with 32nM SN-38 for 4 days and then incubated for 4 days. Most of the MDA-MB-231 cells were transformed into senescent cells.

	Source	J Immunol Res (2018). Figure 1. SN-38
	Method	flow cytometry
	Cell Lines	NB cell lines
	Concentrations	1 nM
	Incubation Time	24 hours
	Results	Cisplatin at 2 μM, etoposide at 0.1 μM, irinotecan at 1 nM, and topotecan at 10nM induced apoptosis of all NB cell lines after 48 hours of treatment, with the exception of SK-N-AS treated with the first three drugs and SK-N-BE(2)c treated with all four drugs

Protocol

Cell Experiment
Cell lines	A-172, U-87, and LA-567
Preparation method	MTT assay
Concentrations	0 -1000 nM
Incubation time	48 h

Animal Experiment
Animal models	Nontumor-bearing mice
Formulation	dissolved in DMSO (1 mg/mL)
Dosages	1 mg/kg
Administration	i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information

References

Disposition of irinotecan and SN-38 following oral and intravenous irinotecan dosing in mice.
Stewart CF, et al. Cancer Chemother Pharmacol. 1997;40(3):259-65. PMID: 9219511.