Sapanisertib [1224844-38-5]
Referencia T1838-5mg
embalaje : 5mg
Marca : TargetMol
Sapanisertib
(Synonyms: TAK-228, MLN0128, INK 128) Copy Product Info
Sapanisertib (INK 128) is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.
Cas No. 1224844-38-5
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Purity:99.67%
Color:White to Red
COA HNMR LCMS
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Sapanisertib (INK 128) is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity. |
| Targets & IC50 | PI3Kγ:221 nM, PI3Kα:219 nM, mTOR:1.4 nM(Ki), PI3Kδ:230 nM, PI3Kβ:5.293 μM |
| In vitro | Administering INK 128 orally on a daily basis to various transplant model systems inhibits angiogenesis and tumor growth. Daily treatment of the ZR-75-1 breast cancer xenograft model with 0.3 mg/kg of INK 128 demonstrated a suppressive effect on tumor growth. |
| In vivo | INK 128 functions as a dual inhibitor of TORC1/2, suppressing the phosphorylation of TORC1's downstream substrates S6 and 4EBP1, while selectively inhibiting the phosphorylation of AKT on Ser473, a downstream substrate of TORC2. It exhibits enzymatic inhibitory activity against mTOR, presenting over 100-fold selectivity towards PI3K kinases. Moreover, INK 128 effectively inhibits cell lines resistant to rapamycin and pan-PI3K inhibitors. |
| Synonyms | TAK-228, MLN0128, INK 128 |
| Kinase Assay | mTOR activity is assayed using LanthaScreen Kinase kit reagents. PI(3)K α, β, γ and δ activity are assayed using the PI(3)K HTRF assay kit. The concentration of INK128 necessary to achieve inhibition of enzyme activity by 50% (IC50) is calculated using concentrations ranging from 20 μM to 0.1 nM (12-point curve). IC50?values are determined using a nonlinear regression model. |
| Cell Research | PC3 cells are treated with the appropriate drug for 48 h, and proliferation is measured using CellTiter-Glo Luminescent reagent. The concentration of INK128 necessary to achieve inhibition of cell growth by 50% (IC50) is calculated using concentrations ranging from 20.0 μM to 0.1 nM (12-point curve). |
| Molecular Weight | 309.33 |
| Formula | C15H15N7O |
| Cas No. | 1224844-38-5 |
| Smiles | CC(C)n1nc(-c2ccc3oc(N)nc3c2)c2c(N)ncnc12 |
| Relative Density. | 1.64 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 2 mg/mL (6.47 mM), Sonication is recommended. DMSO: 60 mg/mL (193.97 mM), Sonication is recommended.  H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.47 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 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||