Temsirolimus CCI-779 NSC 683864 Cas 162635-04-3

Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay.

In the absence of FKBP12, Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM. Temsirolimus treatment at nanomolar concentrations (10 nM to <5 μM) displays a modest and selective antiproliferative activity via FKBP12-dependent mechanism, but can completely inhibit the proliferation of a broad panel of tumor cells at low micromolar concentrations (5-15 μM), involving FKBP12-independent suppression of mTOR signaling. Temsirolimus treatment at micromolar but not nanomolar concentrations (20 μM) causes a marked decline in global protein synthesis and disassembly of polyribosomes, accompanied by rapid increase in the phosphorylation of translation elongation factor eEF2 and the translation initiation factor eIF2A. Temsirolimus inhibits the phosphorylation of ribosomal protein S6, more potently in PTEN-positive DU145 cells than in PTEN-negative PC-3 cells, and inhibits cell growth and clonogenic survival of both cells in a concentration-dependent manner. Temsirolimus (100 ng/mL) potently inhibits proliferation and induces apoptosis in primary human lymphoblastic leukemia (ALL) cells.

Properties:

Appearance & Physical State: white crystalline powder

Density: 1.2g/cm3

Boiling Point: 1048.4ºC at 760mmHg

Melting Point: 99-101ºC

Flash Point: 587.8ºC

Refractive Index: 1.553

Vapor Pressure: 0mmHg at 25°C

Related Products:

Everolimus; PI-103; Torin 1; PF-04691502; Apitolisib; Torin 2; BGT226; Palomid 529; Deforolimus; KU-0063794; Rapamycin; Tacrolimus; Dactolisib

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[2] Wu L, et al. Cancer Res, 2005, 65(7), 2825-2831.

[3] Teachey DT, et al. Blood, 2006, 107(3), 1149-1155.