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MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM. Proteasome activity was significantly inhibited in both blood and tumor following a single dose of MLN2238 administered IV at 14 mg/kg or SC at 4 mg/kg. It is active in preclinical models of lymphoma, and that MLN2238 has antitumor activity in a model of lymphoma that is refractory to bortezomib treatment.
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Source | Cell Death Dis (2018). Figure 5. MLN2238 |
| Method | MTS assay | |
| Cell Lines | HepG2 a, Hep3B b, and SNU475 c cells | |
| Concentrations | 0-1000 nM | |
| Incubation Time | 24, 48, and 72 h | |
| Results | Fig. 1d shows that after 48 h MLN2238 significantly inhibited HCC cell proliferation according to the drug concentration. |
| Molecular Weight | 361.03 |
| Formula | C14H19BCl2N2O4 |
| CAS Number | 1072833-77-2 |
| 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 |
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