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PI3K/mTOR-IN-20 is a selective dual inhibitor of PI3K/mTOR. It demonstrates nanomolar anti-proliferative effects in MRC-5 and Mlg2908 cells with IC50 values of 0.380 and 0.090 μM, respectively. In a Bleomycin-induced pulmonary fibrosis model, PI3K/mTOR-IN-20 reduces Ashcroft scores, decreases hydroxyproline content and collagen deposition, downregulates fibrosis-related protein expression, and aids in the repair of lung tissue structure. This compound exhibits good safety, as indicated by stable weight recovery in mice without significant hepatic or renal toxicity. PI3K/mTOR-IN-20 is useful for research on pulmonary fibroblasts.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | PI3K/mTOR-IN-20 is a selective dual inhibitor of PI3K/mTOR. It demonstrates nanomolar anti-proliferative effects in MRC-5 and Mlg2908 cells with IC50 values of 0.380 and 0.090 μM, respectively. In a Bleomycin-induced pulmonary fibrosis model, PI3K/mTOR-IN-20 reduces Ashcroft scores, decreases hydroxyproline content and collagen deposition, downregulates fibrosis-related protein expression, and aids in the repair of lung tissue structure. This compound exhibits good safety, as indicated by stable weight recovery in mice without significant hepatic or renal toxicity. PI3K/mTOR-IN-20 is useful for research on pulmonary fibroblasts. |
| In vitro | PI3K/mTOR-IN-20 (compound 11) exhibits nanomolar antiproliferative activity against MRC-5 and Mlg2908 cells with IC50 values of 0.38 μM and 0.09 μM, respectively. At a concentration of 1 μM, it effectively inhibits mTOR and class I PI3K isoforms (α, β, and γ), while showing weaker inhibition on PI3Kδ. The inhibition rates for PI3Kα, PI3Kβ, PI3Kγ, and mTOR are 94.89%, 79.24%, 42.60%, and 42.99%, respectively. Additionally, PI3K/mTOR-IN-20 (1 μM, 48-hour treatment) effectively inhibits PI3K activity and reduces fibroblast activation in MRC-5 cells. |
| In vivo | PI3K/mTOR-IN-20 (compound 11) administered at 15 mg/kg via intraperitoneal injection daily for 11 days demonstrates significant antifibrotic effects in a Bleomycin (BLM)-induced pulmonary fibrosis mouse model. It reduces collagen deposition, restores lung structure, inhibits fibrotic processes, and improves physiological parameters with favorable safety. Additionally, PI3K/mTOR-IN-20 (15-60 mg/kg, intraperitoneal injection, once daily for 3 days) exhibits no significant hepatotoxicity or nephrotoxicity in the same model. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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.
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.
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