Temsirolimus (CCI-779) inhibited the growth of xenografts derived from both cell lines with greater effects against PC-3 than DU145 tumors. Temsirolimus caused mild myelosuppression. The activity of mitoxantrone or docetaxel was limited, but CCI-779 given between courses of chemotherapy increased growth delay of PC-3 xenografts. High-dose temsirolimus inhibits mTOR signaling through an FKBP12-independent mechanism that leads to profound translational repression. This distinctive high-dose compound effect could be directly related to the antitumor activities of temsirolimus and other rapalogues in human cancer patients. The rapamycin analogue CCI-779 is an important new agent to investigate in the treatment of human brain tumors, particularly PNET/MB. The rapamycin analogue temsirolimus improved performance on four different behavioral tasks and decreased aggregate formation in a mouse model of Huntington disease.
Mol Cell. 2018 Dec 3.
Phosphorylated RB Promotes Cancer Immunity by Inhibiting NF-κB Activation and PD-L1 Expression.
Temsirolimus purchased from AbMole
Cell Death and Disease. 2018 Jan 26;9:137-52.
Downregulation of MCL-1 and upregulation of PUMA using mTOR inhibitors enhance antitumor efficacy of BH3 mimetics in triple-negative breast cancer
Temsirolimus purchased from AbMole
J Agric Food Chem. 2017 Mar 15;65(10):2089-2099.
10-Gingerol, a Phytochemical Derivative from “Tongling White Ginger”, Inhibits Cervical Cancer: Insights into the Molecular Mechanism and Inhibitory Targets
Temsirolimus purchased from AbMole
Cell Experiment | |
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Cell lines | A549, H157, H460, H446, HCT116, HT29, SW480, DLD1, Caco2, LNCap, DU145, MDA468, MDA231, HEK293, and PC3-MM2 |
Preparation method | Exposing cells to various concentrations of Temsirolimus for 72 hours. After treatment, using CellTiter AQ assay kit to determing viable cell densities by MTS dye conversion. |
Concentrations | Dissolved in DMSO, final concentrations ~20 μM |
Incubation time | 72 hours |
Animal Experiment | |
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Animal models | Female athymic nude mice injected s.c. with DAOY, or U251 cells |
Formulation | Prepared in 100% EtOH as a 50 mg/mL stock solution, and diluted in 5% Tween 80 and 5% polyethylene glycol 400 |
Dosages | 20 mg/kg |
Administration | Injection daily 5 times per week |
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Molecular Weight | 1030.29 |
Formula | C56H87NO16 |
CAS Number | 162635-04-3 |
Purity | 100.00% |
Solubility | DMSO ≥180 mg/mL Ethanol ≥180 mg/mL |
Storage | at -20°C |
A new pharmacologic action of CCI-779 involves FKBP12-independent inhibition of mTOR kinase activity and profound repression of global protein synthesis.
Shor B, et al. Cancer Res. 2008 Apr 15;68(8):2934-43. PMID: 18413763.
Effects of the mammalian target of rapamycin inhibitor CCI-779 used alone or with chemotherapy on human prostate cancer cells and xenografts.
Wu L, et al. Cancer Res. 2005 Apr 1;65(7):2825-31. PMID: 15805283.
Inhibition of mTOR induces autophagy and reduces toxicity of polyglutamine expansions in fly and mouse models of Huntington disease.
Ravikumar B, et al. Nat Genet. 2004 Jun;36(6):585-95. PMID: 15146184.
Antitumor activity of the rapamycin analog CCI-779 in human primitive neuroectodermal tumor/medulloblastoma models as single agent and in combination chemotherapy.
Geoerger B, et al. Cancer Res. 2001 Feb 15;61(4):1527-32. PMID: 11245461.
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