Wortmannin-Rapamycin Conjugate

Product Name: Wortmannin-Rapamycin Conjugate
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
Formula Weight: 1598.99
MOL File: 1067892-47-0.mol

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Wortmannin-Rapamycin Conjugate Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 13671
Product name: Wortmannin-Rapamycin Conjugate
Purity: ≥98%
Packaging: 500μg
Price: $152
Updated: 2024/03/01

Cayman Chemical

Product number: 13671
Product name: Wortmannin-Rapamycin Conjugate
Purity: ≥98%
Packaging: 1mg
Price: $288
Updated: 2024/03/01

Cayman Chemical

Product number: 13671
Product name: Wortmannin-Rapamycin Conjugate
Purity: ≥98%
Packaging: 5mg
Price: $1204
Updated: 2024/03/01

AK Scientific

Product number: 1384EN
Product name: 8-O-[(1S,3Ar,6E,9S,9aR,10R,11aS)-10-acetyloxy-6-[[3-(dimethylamino)propyl-methylamino]methylidene]-5-hydroxy-9-(methoxymethyl)-9a,11a-dimethyl-4,7-dioxo-2,3,3a,9,10,11-hexahydro-1H-indeno[4,5-h]isochromen-1-yl]1-O-[(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16Z,18R,19R,21R,23S,24Z,26Z,28Z,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl]octanedioate
Packaging: 5mg
Price: $1439
Updated: 2021/12/16

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Wortmannin-Rapamycin Conjugate Chemical Properties,Usage,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 Preparation Products And Raw materials

Raw materials

Preparation Products

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Wortmannin-Rapamycin Conjugate Suppliers

China 14 United States 3 Global 17

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1067892-47-0, Wortmannin-Rapamycin ConjugateRelated Search:

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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