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Temsirolimus

Cat. No. M3722
Temsirolimus Structure
Synonym:

CCI-779

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 260 In stock
100mg USD 450 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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
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
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 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.

Chemical Information
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
Customer Product Validations & Biological Datas
Source APMIS.m (2017). Figure 7. temsirolimus (Abmole Bioscience Inc. Houston, TX, USA)
Method Western blot
Cell Lines HeLa cells
Concentrations
Incubation Time
Results In addition, exposure with deguelin and temsirolimus could weaken the inhibitory attributes of 10-G on the expression of p-AKT and p-mTOR.
Rating
Product Citations
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Temsirolimus, CCI-779 supplier, mTOR, inhibitors

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