Temsirolimus (Synonyms: Torisel;CCI-779;CCI 779;CCI779)

Cell lines

PC-3 and DU145 cells

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.

Reaction Conditions

100 nM, 3 days

Applications

The growth and colony-formation of both cell lines were inhibited in a concentration-dependent manner by CCI-779. Following a 3-day exposure to 100 nmol/L CCI-779, the numbers of colony-forming PC-3 and DU145 cells were 0.18 ± 0.09 and 0.37 ± 0.03, respectively, compared with controls.

Animal models

Nude mice bearing DAOY xenografts

Dosage form

Intraperitoneal injection, 20 mg/kg, daily 3 5 for 1, 2 or 4 weeks or 100 mg/kg on days 1 and 12

Applications

CCI-779 administered at 20 mg/kg 5 days/week for 1 and 2 weeks yielded 1.6- and 2.4-fold delayed tumor growth. Time to reach 5-fold tumor volume was significantly greater in animals treated for 1 week or 2 weeks compared with control animals. Retreatment of large tumors with CCI-779 for 2 weeks (20 mg/kg i.p. 5 days/week on days 29 to 42) restored growth inhibition but did not yield tumor regression. Treatment with CCI-779 (20 mg/kg i.p.) 5 days/week for 4 weeks delayed time to reach 5-fold pretreatment volume by 174% compared with controls.

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] Wu L, Birle D C, Tannock I F. Effects of the mammalian target of rapamycin inhibitor CCI-779 used alone or with chemotherapy on human prostate cancer cells and xenografts. Cancer research, 2005, 65(7): 2825-2831.

[2] Geoerger B, Kerr K, Tang C B, et al. Antitumor activity of the rapamycin analog CCI-779 in human primitive neuroectodermal tumor/medulloblastoma models as single agent and in combination chemotherapy[J]. Cancer research, 2001, 61(4): 1527-1532.