Figure 7
Figure 7. Pim inhibition suppresses MM growth in mouse xenograft model. (A) Scid/bg mice were administered a single oral dose of LGB321 at 10, 20, 50, and 100 mg/kg, and LGB321 levels were detected in plasma collected from each animal at 1, 8, and 24 hours post dose (n = 3 per time point). (B) Pharmacodynamics were measured by assessing modulation of p-BAD and p-S6RP in the lysate of subcutaneous KMS-11.luc tumors from animals given a single dose of 10, 20, 50, or 100 mg/kg of LGB321, at 1, 8, or 24 hours post dosing (n = 3 per time point). Both phosphorylated and total forms of BAD and S6RP were detected by electrochemiluminescence, and a ratio was calculated to express percent inhibition of the phosphorylated form normalized to vehicle-treated tumors. (C) Mice bearing subcutaneous KMS-11.luc tumors were dosed by oral gavage with vehicle or LGB321 at daily doses of 20, 40, or 100 mg/kg per day (n = 9 per group). A dose-dependent inhibition of tumor growth was demonstrated, and tumor stasis was achieved with 100 mg/kg per day. *P < .05. (D) Body weight of animals in all dosing groups was measured and calculated to express the changes within the period of study. SEM, standard error of the mean.

Pim inhibition suppresses MM growth in mouse xenograft model. (A) Scid/bg mice were administered a single oral dose of LGB321 at 10, 20, 50, and 100 mg/kg, and LGB321 levels were detected in plasma collected from each animal at 1, 8, and 24 hours post dose (n = 3 per time point). (B) Pharmacodynamics were measured by assessing modulation of p-BAD and p-S6RP in the lysate of subcutaneous KMS-11.luc tumors from animals given a single dose of 10, 20, 50, or 100 mg/kg of LGB321, at 1, 8, or 24 hours post dosing (n = 3 per time point). Both phosphorylated and total forms of BAD and S6RP were detected by electrochemiluminescence, and a ratio was calculated to express percent inhibition of the phosphorylated form normalized to vehicle-treated tumors. (C) Mice bearing subcutaneous KMS-11.luc tumors were dosed by oral gavage with vehicle or LGB321 at daily doses of 20, 40, or 100 mg/kg per day (n = 9 per group). A dose-dependent inhibition of tumor growth was demonstrated, and tumor stasis was achieved with 100 mg/kg per day. *P < .05. (D) Body weight of animals in all dosing groups was measured and calculated to express the changes within the period of study. SEM, standard error of the mean.

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