Molecular Formula | C20H23BCl2N2O9 |
Molar Mass | 517.12 |
Density | 1.47 |
Melting Point | >227°C (dec.) |
Solubility | DMSO (Slightly), Methanol (Slightly, Heated, Sonicated) |
Appearance | Solid |
Color | White to Off-White |
pKa | 1.92±0.20(Predicted) |
Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
In vitro study | Compared with bortezomib, MLN9708 has a shorter separation half-life and higher pharmacokinetics, pharmacodynamics, and anticancer activity. MLN9708 is a second-generation small molecule proteasome inhibitor for the treatment of a variety of human malignant gliomas. After contact with aqueous solution and plasma, MLN9708 is rapidly hydrolyzed to mln2238. MLN2238 is the biologically active form of mln9708. MLN2238 is a nitrogen-capped dipeptide leucine boronic acid, which inhibits the chymotrypsin (β5) hydrolysis site of the 20S proteasome, with an IC50 of 3.4 nM and a K I value of 0.93 nM. At higher concentrations, MLN2238 also inhibited the caspase-like hydrolysis (β1) site and the trypsin-like hydrolysis (β2) site of the 20S proteasome with IC50 of 31 nM and 3.5 µm, respectively. MLN2238 is a potent and selective reversible inhibitor of the proteasome, and this reversibility is time-dependent. |
In vivo study | MLN9708 has extremely high anticancer activity in solid tumors and preclinical xenografts in the blood. Recent preclinical pharmacology studies have shown that MLN9708 acts on transplanted tumors with a shorter isolation half-life, higher pharmacokinetics, pharmacodynamics, and anti-cancer activity. MLN9708 has anticancer activity on a variety of transplanted tumors. |
Safety Description | 24/25 - Avoid contact with skin and eyes. |
HS Code | 29329990 |