Wortmannin-Rapamycin Conjugate

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Cat No: 13671

Biochemicals - Kinase Inhibitors

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.{16465,16931} Wortmannin-rapamycin conjugat...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

1-(4S,4aR,5R,6aS,7S,9aR,E)-1-(((3-(dimethylamino)propyl)(methyl)amino)methylene)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate 8-(7E,15E,17E,19E)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34aS-hexadecahydro-9R,27-dihydroxy-3S-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10R,21S-dimethoxy-6R,8,12R,14S,20,26R-hexamethyl-23S,27R-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone octanedioate

Correlated keywords:

phosphoinositide 3-kinases PI3K kinases three 3 mammalian targets rapamycins mTOR cancers inhibitors inhibits inhibitions TORC1 TORCs TORC-1 1 one prodrugs pro-drugs linkers linkage HT29 HT-29 colon tumors A498 A-498 As 498 renal tumors VEGF bevacizumab

Product Overview:
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.{16465,16931} Wortmannin-rapamycin conjugate consists of analogs of 17-hydroxy wortmannin and rapamycin conjugated via a prodrug linker.{17899} 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.{17899} 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.{17899}

Size	500 µg
Shipping	dry ice
CAS Number	1067892-47-0
Molecular Formula	C₈₈H₁₃₁N₃O₂₃
SMILES	O=C(O[C@H]1[C@H](OC)C[C@H](C[C@@H](C)[C@@](CC([C@H](C)/C=C(C)/[C@@H](O)[C@@H](OC)C([C@H](C)C[C@H](C)/C=C/C=C/C=C(C)/[C@@H](OC)C[C@](O2)([H])CC[C@@H](C)[C@]2(O)C3=O)=O)=O)([H])OC([C@]4([H])CCCCN4C3=O)=O)CC1)CCCCCCC(O[C@H]5CC[C@]6([H])[C@]5(C)C[C@@H](OC(C)=
Molecular Weight	1598,9
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2919.90
UNSPSC code	12352100

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