Description
Temsirolimus (Torisel) can inhibit mTOR with IC50 of 1.76 uM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C56H87NO16
Chemical Name
Rapamycin, 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate]
Solubility
DMSO 75 mg/mL Water 1 mg/ml Ethanol 75 mg/mL
In vitro
As a mTOR inhibitor, temsirolimus (cell cycle inhibitor-779, CCI 779) can inhibit mTOR with IC50 of 1.76 uM. Temsirolimus (cell cycle inhibitor-779, CCI 779) is an ester analogue of sirolimus for the treatment of cancer, multiple sclerosis and rheumatoid arthritis. Temsirolimus binds to the cytosolic protein, FKBP, which subsequently inhibits mTOR (mammalian target of rapamycin). Inhibition of mTOR blocks a number of signal transduction pathways that suppress translation of several key proteins regulating the cell cycle. By inhibiting mTOR, temsirolimus lead to a cell cycle block at the G1 phase.
In vivo
In animal models of human cancers, temsirolimus inhibited the growth of a diverse range of cancer types even when an intermittent dosing schedule was used. Temsirolimus also appears to have potential for the blockade of inflammatory responses associated with autoimmune and rheumatic diseases by inhibiting T-cell proliferation.
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