| Identification | Back Directory | [Name]
Wortmannin-Rapamycin Conjugate | [CAS]
1067892-47-0 | [Synonyms]
ATASUAOFUAOSAN-NVEIXTJJSA-N
Wortmannin-Rapamycin Conjugate
Rapamycin, 42-[8-[(1E,4S,4aR,5R,6aS,7S,9aR)-5-(acetyloxy)-1-[[[3-(dimethylamino)propyl]methylamino]methylene]-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydro-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxocyclopenta[5,6]naphtho[1,2-c]pyran-7-yl] octanedioate] | [Molecular Formula]
C88H131N3O23 | [MOL File]
1067892-47-0.mol | [Molecular Weight]
1598.99 |
| Hazard Information | Back Directory | [Description]
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. |
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| Company Name: |
BOC Sciences
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16314854226 |
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www.bocsci.com |
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