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Rapalink-1

Name: Rapalink-1
Brand: TargetMol
SKU: TP2288
Rating: 4.5 (1 reviews)

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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

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Catalog No. TP2288Cas No. 1887095-82-0

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$1,200	7-10 days	7-10 days
10 mg	$2,235	7-10 days	7-10 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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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 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,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 160 mg/mL (89.68 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 5 mg/mL (2.8 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.5605 mL	2.8025 mL	5.6049 mL	28.0247 mL
5 mM	0.1121 mL	0.5605 mL	1.1210 mL	5.6049 mL
10 mM	0.0560 mL	0.2802 mL	0.5605 mL	2.8025 mL
20 mM	0.0280 mL	0.1401 mL	0.2802 mL	1.4012 mL
50 mM	0.0112 mL	0.0560 mL	0.1121 mL	0.5605 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc