Wortmannin-Rapamycin Conjugate Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Phosphoinositide 3-
kinase (PI3K) and mammalian target of rapamycin (mTOR) act synergistically in promoting cancer. Wortmannin is a potent inhibitor of PI3K enzymes, while rapamycin blocks mTOR Complex 1 TORC1. Wortmannin-
rapamycin conjugate consists of analogs of 17-
hydroxy wortmannin and rapamycin conjugated
via a prodrug linker. Hydrolysis of the prodrug linker
in vivo releases the inhibitors. The wortmannin-
rapamycin conjugate inhibits the growth of HT-29 colon tumors and A498 renal tumors in mice better than rapamycin alone. Also, the conjugate, when given in combination with the VEGF-
blocker bevacizumab, produces substantial regression of larger A498 tumors. Finally, the wortmannin-
rapamycin conjugate is tolerated better than an equivalent mixture of the inhibitors.
Wortmannin-Rapamycin Conjugate Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte