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.
|Source||Cell Death Dis (2018). Figure 5. MLN2238|
|Cell Lines||HepG2 a, Hep3B b, and SNU475 c cells|
|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.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
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