IPI-145 is a novel and selective PI3K δ/γ inhibitor with IC50 of 23 pM and 243 pM, respectively. IPI-145 prevents the activation of the PI3K delta/gamma-mediated signaling pathways which may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. IPI-145 suppresses murine/human B-cell proliferation with EC50 of 0.5 nM/0.5 nM and also inhibits human T-cell proliferation with EC50 of 9.5 nM. IPI-145 was well tolerated and clinically active in a broad range of malignancies, including iNHL. IPI-145 (10 mg/kg) demonstrates dose-dependent effect in rat collagen induced arthritis (CIA) model.
|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 80 mg/mL|
|Source||Blood (2014). Figure 1. IPI-145|
|Cell Lines||CLL cells|
|Concentrations||0.01 to 1 μM|
|Incubation Time||24 h|
|Results||Cell viability was measured every 24 hours; 0.25 to 5 μM IPI-145 exhibited concentration and timedependent induction of cytotoxicity in CLL.|
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