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
Temsirolimus results in significant drop in global protein synthesis and disassembly of polyribosomes with speedy growth in the phosphorylation of translation elongation factor eEF2 and the translation initiation factor eIF2A. Compared with the effect in PTEN-negative PC-3 cells, Temsirolimus exhibits greater effect in inhibition of the phosphorylation of ribosomal protein S6 in PTEN-positive DU145 cells. And in a concentration-dependent manner, cell growth and clonogenic survival of both cells are inhibited by Temsirolimus. Potent proliferation inhibition and apoptosis inducing in primary human lymphoblastic leukemia (ALL) cells are produced by Temsirolimus (100 ng/mL) as well.
* Above data is for reference only. Accuracy is not confirmed.

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.
* Above data is for reference only. Accuracy is not confirmed.

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
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

Documentation

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