| Name | Sapanisertib |
| 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. |
| 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). |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 2 mg/mL (6.46 mM)
DMSO : 18.33 mg/mL (59.27 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | MLN 0128 | INK128 | inhibit | TAK 228 | INK-128 | Sapanisertib | TAK228 | Autophagy | Mammalian target of Rapamycin | MLN-0128 | mTOR | Inhibitor |
| Inhibitors Related | Stavudine | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
