Sapanisertib

SKU: orb1307349

Description

Sapanisertib

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1224844-38-5
• MW: 309.33
• Purity: 99.67%
• Formula: C₁₅H₁₅N₇O
• SMILES: CC(C)n1nc(-c2ccc3oc(N)nc3c2)c2c(N)ncnc12
• Target: mTOR,Autophagy,PI3K
• Solubility: DMSO:60 mg/mL (193.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.47 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:2 mg/mL (6.47 mM)

Bioactivity

• Target IC50:
  PI3Kα:219 nM|PI3Kβ:5.293 μM|PI3Kγ:221 nM|mTOR:1.4 nM(Ki)|PI3Kδ:230 nM
• 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.
• 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.
• 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).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, Mammalian target of Rapamycin, Inhibitor, INK 128, INK128, INK-128, MLN0128, MLN-0128, MLN 0128, mTOR, inhibit, TAK 228, TAK228, TAK-228, Sapanisertib, PI3Kα, PI3Kδ, PI3Kγ

Compound Identifiers

PubChem CID

45375953