Daun02

Cell lines

Panc02, MCF-7, T47-D, PC3, DU145 and LNCap cells (transduced to express E.coli β-gal)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

EC50: 0.5 to 5.5 μM, 24 hours

Applications

The prodrug Daun02 was converted to daunomycin by the β-galactosidase. It inhibited the cell viability with EC50 values of 1.5, 3.5, 0.5, 5.0, 5.5, 5.0 for Panc02, MCF-7, T47-D, PC3, DU145 and LNCap tumor cells, respectively.

Animal models

Male athymic BALB/c mice implanted with β-gal-transduced Panc02 cells

Dosage form

Intraperitoneal injection, 200 mg/kg

Application

None of the tumors responded to treatment with intraperitoneal Daun02. The dose for Daun02 was the highest tested due to the limited water solubilityof the compound. At this dose, the animals did not appear to experience anytoxicityas evidenced bynormal physical and behavioral characteristics and continued weight gain. It may be due to the less distribution and the poor penetrability of Daun02 across cell membranes.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] David Farquhar, Bih Fang Pan, Mamoru Sakurai, AjitGhosh, Craig A. Mullen, J. Arly Nelson. Suicide gene therapy using E.Coli β-galactosidase. Cancer ChemotherPharmacol.2002, 50: 65–70.