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Rapalink-1
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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
😃Good
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $581 | 7-10 days | |
| 25 mg | $1,650 | 7-10 days |
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Product Introduction
Bioactivity
Chemical Properties
| 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] |
| Molecular Weight | 1784.14 |
| Formula | C91H138N12O24 |
| Cas No. | 1887095-82-0 |
| Smiles | NC1=C2C(=NN(CCCCNC(CCOCCOCCOCCOCCOCCOCCOCCOCCN3C=C(COCCO[C@H]4[C@H](OC)C[C@H](C[C@@H](C)[C@]5(OC(=O)[C@]6(N(C(=O)C(=O)[C@]7(O)O[C@@](CC[C@H]7C)(C[C@H](OC)\C(\C)=C\C=C\C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(/C)=C\[C@@H](C)C(=O)C5)[H])CCCC6)[H])[H])CC4)N=N3)=O)C2=NC=N1)C=8C=C9C(=CC8)OC(N)=N9 |
| Relative Density. | 1.30 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | keep 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
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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