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Sapanisertib (MLN0128)
| Product Name | Sapanisertib (MLN0128) |
| Price: | Inquiry |
| Catalog No.: | CN00466 |
| CAS No.: | 1224844-38-5 |
| Molecular Formula: | C15H15N7O |
| Molecular Weight: | 309.33 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | Nc1oc2c(n1)cc(cc2)c1nn(c2c1c(N)ncn2)C(C)C |
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| Description | Sapanisertib (INK-128) is a ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase. |
| Target | mTOR:1 nM (IC50) mTORC1 mTORC2 PI3Kα:219 nM (IC50) PI3Kβ:5.293 μM (IC50) PI3Kδ:230 nM (IC50) PI3Kγ:221 nM (IC50) Autophagy |
| In Vitro | Sapanisertib (INK-128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases[1]. Sapanisertib (INK-128) selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. Sapanisertib (INK-128) decreases the invasive potential of PC3 prostate cancer cells. Furthermore, Sapanisertib (INK-128) inhibits cancer cell migration starting at 6 h of treatment, precisely correlating with when decreases in the expression of pro-invasion genes are evident, but preceding any changes in the cell cycle or overall global protein synthesis[2]. |
| In Vivo | In a ZR-75-1 breast cancer xenograft model, Sapanisertib (INK-128) shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day[1]. 4EBP1 and p70S6K1/2 phosphorylation is completely restored to wild-type levels after treatment with INK128 in PtenL/L mice. Sapanisertib (INK-128) treatment results in a 50% decrease in prostatic intraepithelial neoplasia (PIN) lesions in PtenL/L mice and induces programmed cell death in multiple cancer cell lines in mice[2]. |
| Cell Assay | PC3 cells are treated with the appropriate drug for 48 h, and proliferation is measured using CellTiter-Glo Luminescent reagent. The concentration of Sapanisertib (INK-128) 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). |
| Animal Admin | Nude mice are inoculated subcutaneously in the right subscapular region with 5×106 MDA-MB-361 cells. After tumours reach a size of 150-200 mm3, mice are randomLy assigned into vehicle control or treatment groups. Sapanisertib (INK-128) is formulated in 5% polyvinylpropyline, 15% NMP, 80% water and administered by oral gavage at 0.3 mg/kg and 1 mg/kg daily. |
| Density | 1.6±0.1 g/cm3 |
| Boiling Point | 598.8±60.0 °C at 760 mmHg |
| Flash Point | 315.9±32.9 °C |
| Exact Mass | 309.133820 |
| PSA | 121.67000 |
| LogP | 1.95 |
| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
| Storage condition | -20°C |