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Temsirolimus, also known as CCI-779, an inhibitor of mTOR, is a derivative and prodrug of Rapamycin. It is often used in the treatment of renal cell carcinoma (RCC). Temsirolimus also has the ability to inhibit the growth of wide range of tumor cells. In the absence of FKBP12, Temsirolimus has potent effects in inhibiting mTOR kinase activity.
CAS No. |
159351-69-6 |
Purity |
99.10% |
Target |
mTOR |
IC50 |
1.76 μM |
In Vitro |
Similar to Rapamycin, with IC50 of 1.76 μM, Temsirolimus has potent inhibitory effects in mTOR kinase activity in the absence of FKBP12. At low micromolar concentrations (5-15 μM), Temsirolimus produces full inhibition of prliferation of a collection of tumor cells, while at 10 nM to <5 μM, it shows a good and selective activity of anti-proliferation. At micromolar rather than nanomolar concentrations, the treatment by |
In Vivo |
Proliferation of both prostate cancer xenografts can be inhibited by Temsirolimus (20 mg/kg, i.p.). And Temsirolimus also inhibits the growth of PC-3 tumors dose-dependently with a greater inhibition effect than for DU145 tumors. In the NOD/SCID xenograft models with human ALL,with a daily 10mg/kg treatment, Temsirolimus produces reduction in peripheral blood blasts and in splenomegaly. Compared with controls, by administration of Temsirolimus (20 mg/kg, i.p. 5 days/week), the increase of DAOY xenografts are delayed by 160% 1 week later and 240% 2 weeks later. 37% regression of tumor volume in a week is achieved by a single high-dose treatment of Temsirolimus (100 mg/kg, i.p). A 2-week treatment of Temsirolimus is also able to delay the proliferation of rapamycin-resistant U251 xenografts by 148%. In a mouse model of Huntington disease, aggregate formation is declined through mTOR inhibition by Temsirolimus. |
Formula |
C₅₆H₈₇NO₁₆ |
SMILES |
O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C([C@@H]([C@@H](/C(C)=C/[C@H]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@H]4C[C@H]([C@H](OC(C(C)(CO)CO)=O)CC4)OC)C)=O)=O |
M. Weight |
1030.3 |
Storage |
4°C, protect from light, stored under nitrogen |
Solvent & Solubility |
|
Documentation |
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More Biological Information
http://www.medchemhub.com/