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Rapalink-1

Catalog No. TP2288Cas No. 1887095-82-0

Rapalink-1 is a brain-permeable mTOR inhibitor that inhibits oxidative stress-induced DNA damage and senescence in ethanol-exposed endothelial cells, and inhibits the mTORC1-4E-BP1 pathway in mice.Rapalink-1 is used for the study of prostate cancer due to its anticancer activity.

Rapalink-1

Rapalink-1

Catalog No. TP2288Cas No. 1887095-82-0
Rapalink-1 is a brain-permeable mTOR inhibitor that inhibits oxidative stress-induced DNA damage and senescence in ethanol-exposed endothelial cells, and inhibits the mTORC1-4E-BP1 pathway in mice.Rapalink-1 is used for the study of prostate cancer due to its anticancer activity.
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5 mg$5817-10 days
25 mg$1,6507-10 days
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Product Introduction

Bioactivity
Description
Rapalink-1 is a brain-permeable mTOR inhibitor that inhibits oxidative stress-induced DNA damage and senescence in ethanol-exposed endothelial cells, and inhibits the mTORC1-4E-BP1 pathway in mice.Rapalink-1 is used for the study of prostate cancer due to its anticancer activity.
In vitro
METHODS: U87MG cells were lysed with RapaLink-1 (0.39, 0.78, 1.56, 3.13, 6.25, 12.5 nM, 3 hours) and analyzed by western blot as indicated.
RESULTS: RapaLink-1 selectively inhibited p-RPS6S235/236 and p-4EBP1T37/46 at doses as low as 1.56 nM. mTORC2 targeting p-AKTS473, p-SGK1S78, and p-NDRG1T346 and p-AKTS473 targeting p-GSK3βS9 were inhibited only at high doses. [1]
In vivo
METHODS: BALB/cNU/NU mice were treated with RapaLink-1 (0.4 mg/kg or 4 mg/kg, ip, 15 min) and injected intraperitoneally with 250 mU insulin or saline for 15 min. Mice were sacrificed, and skeletal muscle, liver, and brain were harvested, lysed, and analyzed by Western blotting as indicated.
RESULTS: RapaLink-1 was able to inhibit the expression of p-RPS6S235/236 and p-4EBP1T37/46 in the brain in a concentration-dependent manner, but did not inhibit the expression of the mTORC2 substrate p-AKTS473. [1]
Chemical Properties
Molecular Weight1784.14
FormulaC91H138N12O24
Cas No.1887095-82-0
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 160 mg/mL (89.68 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.5605 mL2.8025 mL5.6049 mL28.0247 mL
5 mM0.1121 mL0.5605 mL1.1210 mL5.6049 mL
10 mM0.0560 mL0.2802 mL0.5605 mL2.8025 mL
20 mM0.0280 mL0.1401 mL0.2802 mL1.4012 mL
50 mM0.0112 mL0.0560 mL0.1121 mL0.5605 mL

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