产品
编 号:F072214
分子式:C24H23F3N4O
分子量:440.46
产品类型
结构图
CAS No: 1210608-43-7
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产品详情
生物活性:
PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.
体内研究:
PIM447 (100 mg/kg; p.o.; 5 times for a week)reduces tumor burden.Animal Model:6-week-old female NOD-SCID-IL-2Rγ?/??(NSG) mice (bearing RPMI-8226-luc cells)
Dosage:100 mg/kg
Administration:p.o.; 5 times for a week
Result:Clearly controlled tumor progression as measured by bioluminescence.?
体外研究:
PIM447 (0.05-10 μM; 24-72 hours) shows antiproliferative effect on the multiple myeloma (MM) cells.PIM447 (10 μM; 6-24 hours) induces apoptosis.PIM447(0.1-10 μM; 48 hours) increases the percentage of cells in the G0-G1 phase and decreases the proliferative phases (S and G2–M) of the cell cycle, in the two cell lines (MM1S and OPM-2 cells) at all doses.