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PI3K/mTOR Inhibitor-1
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Catalog No. T12460Cas No. 1949802-49-6
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM).
PI3K/mTOR Inhibitor-1
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Catalog No. T12460Cas No. 1949802-49-6
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $2,120 | 8-10 weeks | 8-10 weeks | |
| 50 mg | $2,780 | 8-10 weeks | 8-10 weeks | |
| 100 mg | $3,700 | 8-10 weeks | 8-10 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM). |
| Targets&IC50 | PI3Kδ:46 nM, PI3Kα:20 nM, PI3Kβ:376 nM, PI3Kγ:204 nM, mTOR:186 nM |
| In vitro | PI3K/mTOR Inhibitor-1 (Compound 26) is a potent dual PI3K/mTOR inhibitor, demonstrating high inhibitory activity against PI3Kα/β/γ/δ (IC50 = 20/376/204/46 nM) and mTOR (IC50 = 189 nM), potent suppression of AKT phosphorylation (IC50 = 196 nM), and excellent antiproliferative effects on cancer cells. Enzymic data and modeling simulations indicate that a cyclopropyl ring on the C4 sulfone chain and a fluorine on the C6 aminopyridyl moiety are responsible for its maintained PI3K activity and enhanced mTOR potency, respectively. |
| In vivo | PI3K/mTOR Inhibitor-1 (Compound 26) demonstrated superior antiproliferative effects in the HT-29 colorectal carcinoma xenograft model at daily doses of 3.75 and 7.5 mg/kg compared to BKM120 at doses of 15 and 30 mg/kg. |
| Molecular Weight | 407.46 |
| Formula | C18H22FN5O3S |
| Cas No. | 1949802-49-6 |
| Smiles | S(C)(=O)(=O)C1(CC1)C=2C=C(N=C(N2)N3[C@@H](C)COCC3)C=4C(F)=CC(N)=NC4 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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, and a total of 10 animals are to be administered, using a formulation of 
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 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 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 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.
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
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