Wortmannin-Rapamycin Conjugate

TargetMol
Product Code: TAR-T36314
Supplier: TargetMol
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TAR-T36314-1mg1mg£364.00
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TAR-T36314-5mg5mg£1,314.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

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Further Information

Bioactivity:
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.
CAS:
1067892-47-0
Formula:
C88H131N3O23
Molecular Weight:
1599.014
Purity:
0.98
SMILES:
COC[C@H]1OC(=O)C(=CN(C)CCCN(C)C)C2=C(O)C(=O)C3=C([C@@H](C[C@]4(C)[C@H](CC[C@@H]34)OC(=O)CCCCCCC(=O)O[C@@H]3CC[C@@H](C[C@@H](C)[C@@H]4CC(=O)[C@H](C)C=C(C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)C=CC=CC=C(C)[C@H](C[C@@H]5CC[C@@H](C)[C@@](O)(O5)C(=O)C(=O)N5CCCC[C@H]5C(=O)O4)OC)C[C@H]3OC)OC(C)=O)[C@@]12C