• Temsirolimus packaged and labeled in glass vial.

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SKU: T077

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Temsirolimus is a semisynthetic macrocyclic lactone prepared from Rapamycin.  It is a dihydroxymethyl propionic acid ester and analog of Rapamycin. It is prepared by selective acylation of the 42-hydroxy group with a protected bis (dihydromethyl) propionic acid, followed by deprotection.

It is antiproliferative and antiangiogenic mTOR inhibitor.  mTOR protein has a role in integrating environmental signals that affect cell growth and proliferation.  It has anti-neoplastic properties and immune-modulating activity.  Temsirolimus is soluble in ethanol, methanol, DMF and DMSO.

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    Mechanism of Action

    Temsirolimus is a specific inhibitor of mammalian target of rapamycin (mTOR) mTOR Complex 1. (mTORC1). Rapamycin complexes with FK-binding protein (FKBP12) and inhibits mTOR (FRAP, RAFT), a member of the phosphoinositide kinase-related kinase (PIKK) family.

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    Cancer Applications

    Temsirolimus can be used in renal-cell carcinoma (RCC).  The rationale for using mTOR inhibitors to treat malignancies has focused on the direct, growth-inhibitory effects.

    Temsirolimus can enhance anti-tumor immunity.  In an expimental murine model of RCC (RENCA), the combination of an HSP-based cancer vaccine and Temsirolimus was more effective against tumors than either agent alone (ref).   It animal models of tumor vaccines, T enhanced vaccine activity by enhancing effector T-cell function and enhancing production of CD8 memory T cells (Wang et al, 2011).

    Temsirolimus can induce antiproliferative effects by inhibiting mTOR in Bel-7402 liver cancer cells.  Viability tests, and flow cytometry was used to analyze cell cycle after treatment.  It can inhibit mTOR signaling and proliferation in vitro, for a promising strategy for liver cancer (Li et al, 2013).





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    Li S, Liang Y and Wang Z (2013)  The novel mTOR inhibitor CCI-779 (temsirolimus) induces antiproliferative effects through inhibition of mTOR in Bel-7402 liver cancer cells. Cancer Cell Int. 13:30

    Wan X. et al. (2006)  CCI-779 inhibits rhabdomyosarcoma xenograft growth by an antiangiogenic mechanism linked to the targeting of mTOR/Hif-1α/VEGF signaling. Neoplasia 8:394

    Wang Y, Wang X-Y, Subjeck JR, Shikrant PA and Kim HL (2011)  Temsirolimus, an mTOR inhibitor, enhances anti-tumour effects of heat shock protein cancer vaccines. Transl. Ther. 104:643-652 sarcoma xenograft growth by an antiangiogenic mechanism linked to the targeting of mTOR/Hif-1α/VEGF signaling. Neoplasia 8:394

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