SKU: T077  / 
    CAS Number: 162635-04-3

    Temsirolimus

    $87.36 - $305.79

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

    Temsirolimus is an 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. It can be used in kinase phosphatase biology research.

    Temsirolimus is soluble in ethanol, methanol, DMF and DMSO.

    Mechanism of Action Temsirolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing it from interacting with target proteins. 
    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.

    It is surprising that 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.  In animal models of tumor vaccines, Temsirolimus 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).

    References

    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