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INK128 (also known as MLN0128, Sapanisertib) is also an orally bioavailable mTOR inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity. INK128 blocks the phosphorylation of downstream substrates of both TORC1 and TORC2. INK128 (MLN0128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. INK128 interferes with the growth of cell lines which are resistant to rapamycin and pan-PI3K inhibitors. Oral administration of INK128 (MLN0128) inhibits angiogenesis and tumor growth in several xenograft models. In vitro and in vivo studies showed that p-4EBP1 and p-Akt inhibition could be predictive markers of TORC2 inhibition in MM cell lines. Dual TORC1/2 inhibition showed better inhibition of adhesion to BM microenvironmental cells and inhibition of homing in vivo.
Clin Cancer Res. 2018 Nov 15;24(22):5658-5672.
Increased Synthesis of MCL-1 Protein Underlies Initial Survival of EGFR-Mutant Lung Cancer to EGFR Inhibitors and Provides a Novel Drug Target.
INK128 (Sapanisertib) purchased from AbMole
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Source | Clinical Cancer Research (2018 Nov). Figure 2. MLN0128 (Abmole Bioscience) |
| Method | Western blotting | |
| Cell Lines | PC9, HCC4006 and HCC827 cells | |
| Concentrations | 200 nM | |
| Incubation Time | - | |
| Results | Consistently, MCL-1 levels were decreased in both AZD2014 and MLN0128-treated cells. |
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Source | Cancer Biology & Therapy (2015). Figure 1. INK-128 |
| Method | MTT assay | |
| Cell Lines | HT-29 cells | |
| Concentrations | 5, 25 and 100 nM | |
| Incubation Time | 72 h | |
| Results | INK-128 dose-dependently inhibited the number of survival colonies, while increasing the PtdIns staining in HT-29 cells. |
| Molecular Weight | 309.33 |
| Formula | C15H15N7O |
| CAS Number | 1224844-38-5 |
| Solubility (25°C) | DMSO 52 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Maiso P, et al. Blood. Defining the role of TORC1/2 in multiple myeloma.
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All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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