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Wortmannin-Rapamycin Conjugate

Wortmannin-Rapamycin Conjugate Structure
Wortmannin-Rapamycin Conjugate structure
CAS No.
1067892-47-0
Chemical Name:
Wortmannin-Rapamycin Conjugate
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]
CBNumber:
CB42592877
Molecular Formula:
C88H131N3O23
Molecular Weight:
1598.99
MDL Number:
MOL File:
1067892-47-0.mol
MSDS File:
SDS
Last updated:2026-07-27 17:00:41
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Wortmannin-Rapamycin Conjugate Properties

storage temp. Store at -20°C
solubility DMF: 30 mg/ml; DMSO: 20 mg/ml; Ethanol: 5 mg/ml
form A crystalline solid

Wortmannin-Rapamycin Conjugate price More Price(8)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 13671 Wortmannin-Rapamycin Conjugate ≥98% 1067892-47-0 500μg $168 2026-04-30 Buy
Cayman Chemical 13671 Wortmannin-Rapamycin Conjugate ≥98% 1067892-47-0 1mg $317 2026-04-30 Buy
Cayman Chemical 13671 Wortmannin-Rapamycin Conjugate ≥98% 1067892-47-0 5mg $1325 2026-04-30 Buy
ChemScene CS-0146636 Wortmannin-Rapamycin Conjugate 1 1067892-47-0 500??g $362 2026-06-04 Buy
ChemScene CS-0146636 Wortmannin-Rapamycin Conjugate 1 1067892-47-0 1mg $687 2026-06-04 Buy
Product number Packaging Price Buy
13671 500μg $168 Buy
13671 1mg $317 Buy
13671 5mg $1325 Buy
CS-0146636 500??g $362 Buy
CS-0146636 1mg $687 Buy

Wortmannin-Rapamycin Conjugate Chemical Properties, Uses, Production

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.

Uses

Wortmannin-Rapamycin Conjugate 1 (compound 7c) is a furan ring-opened derivative of wortmannin-rapamycin conjugate with potent antitumor activities and a fine water solubility. Wortmannin-Rapamycin Conjugate 1 can inhibit the AKT phosphorylation in the tumor and can be used for cancer research[1].

in vivo

Wortmannin-Rapamycin Conjugate 1 (3,5 mg/kg, i.v., weekly for 13 d) exerts significant antitumor activity on U87MG mouse xenogrgaft model[1].
Wortmannin-Rapamycin Conjugate 1 (15 mg/kg, i.v., 2 h) significantly inhibits the AKT phosphorylation in the tumor of U87MG mouse xenogrgaft model[1].
Wortmannin-Rapamycin Conjugate 1 (15 mg/kg, i.v., weekly for 20 d ) completely inhibits the growth of HT29 colon tumor, a non-sensitive colon tumor model to rapamycin or wortmannin analogues in tumor-bearing mice[1].
Wortmannin-Rapamycin Conjugate 1 (30 mg/kg, i.v., weekly for 38 d ) exerts a substantial regression of larger A498 tumors with 200 μg Bevacizumab (HY-P9906) in A498 tumor-bearing mice[1].

Animal Model:HT29 bearing nude mice[1]
Dosage:15 mg/kg, weekly for 20 d
Administration:Intravenous injection (i.v.)
Result:Showed no significant growth in tumor volume while an equivalent physical mixture of the Rapamycin and Wortmannin derivative was poorly tolerated.

References

[1] Ayral-Kaloustian S, et al. Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates. J Med Chem. 2010 Jan 14;53(1):452-9. DOI:10.1021/jm901427g

Wortmannin-Rapamycin Conjugate synthesis

1067892-18-5
4543-96-8
1067892-47-0
Synthesis of Wortmannin-Rapamycin Conjugate from Ethanamine, N-[(3,5-dichlorophenyl)methylene]-2,2-diethoxy- and N,N,N'-Trimethyl-1,3-propanediamine

Wortmannin-Rapamycin Conjugate Preparation Products And Raw materials

Raw materials

Preparation Products

Wortmannin-Rapamycin Conjugate Suppliers

Global Suppliers ( 17)
Supplier Tel Email Country ProdList Advantage
BOC Sciences 16314854226 info@bocsci.com United States 9909 65
Shanghai Hongye Biotechnology Co. Ltd 400-9205774 400-920-5774 sales@glpbio.cn China 6705 58
TargetMol Chemicals Inc. +1-781-999-5354; +1-00000000000 marketing@targetmol.com United States 32431 58
ChemeGen(Shanghai) Biotechnology Co.,Ltd. 18818260767 sales@chemegen.com China 11123 58
TargetMol Chemicals Inc. 4008200310 15002144251 marketing@tsbiochem.com China 24951 58
Shanghai Yifei Biotechnology Co. , Ltd. 021-65675885 18964387627 customer_service@efebio.com China 11963 58
Supplier Advantage
BOC Sciences 65
Shanghai Hongye Biotechnology Co. Ltd 58
TargetMol Chemicals Inc. 58
ChemeGen(Shanghai) Biotechnology Co.,Ltd. 58
TargetMol Chemicals Inc. 58
Shanghai Yifei Biotechnology Co. , Ltd. 58

View Latest Price from Wortmannin-Rapamycin Conjugate manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Wortmannin-Rapamycin Conjugate pictures 2026-07-27 Wortmannin-Rapamycin Conjugate
1067892-47-0
 $987.00-4260.00 10g TargetMol Chemicals Inc.

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1of2

Wortmannin-Rapamycin Conjugate ATASUAOFUAOSAN-NVEIXTJJSA-N 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] 1067892-47-0 C88H131N3O23