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Sapanisertib

Sapanisertib
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Purity:100%
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Sapanisertib

Catalog No. T1838Cas No. 1224844-38-5
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.
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Pack SizePriceAvailabilityQuantity
1 mg$34In Stock
2 mg$47In Stock
5 mg$77In Stock
10 mg$97In Stock
25 mg$163In Stock
50 mg$247In Stock
100 mg$369In Stock
500 mg$883In Stock
1 mL x 10 mM (in DMSO)$81In Stock
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Product Introduction

Bioactivity
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
PI3Kδ:230 nM, mTOR:1.4 nM(Ki), PI3Kγ:221 nM, PI3Kα:219 nM
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.
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).
AliasTAK-228, MLN0128, INK 128
Chemical Properties
Molecular Weight309.33
FormulaC15H15N7O
Cas No.1224844-38-5
Storage & Solubility Information
StoragePowder: -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)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM3.2328 mL16.1640 mL32.3279 mL161.6397 mL
5 mM0.6466 mL3.2328 mL6.4656 mL32.3279 mL
DMSO
1mg5mg10mg50mg
10 mM0.3233 mL1.6164 mL3.2328 mL16.1640 mL
20 mM0.1616 mL0.8082 mL1.6164 mL8.0820 mL
50 mM0.0647 mL0.3233 mL0.6466 mL3.2328 mL

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