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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
😃Good
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 | Availability | Quantity |
|---|---|---|---|
| 25 mg | $2,120 | 8-10 weeks | |
| 50 mg | $2,780 | 8-10 weeks | |
| 100 mg | $3,700 | 8-10 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 | PI3Kγ:204 nM, mTOR:186 nM, PI3Kβ:376 nM, PI3Kα:20 nM, PI3Kδ:46 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 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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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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