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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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