mTOR inhibitor with anti-cancer activity. Temsirolimus is a semisynthetic macrocyclic lactone prepared from rapamycin by selective acylation of the 42-hydroxy group with a protected bis(dihydromethyl)propionic acid, followed by deprotection. It has anti-angiogenic effects which may contribute to the antitumor activity of temsirolimus observed in breast cancer. Temsirolimus shows synergistic in vivo anti-myeloma effects in combination with dexamethasone in a xenograft model. Temsirolimus is extensively cited in the literature with over 700 citations.
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