产品
编 号:F155168
分子式:C25H30N8O2
分子量:474.56
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.

体内研究:
PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice.

体外研究:
PIM1-IN-1 (Compound 42) exhibits antiproliferative activity, with GI50 of 1.48 μM for melanoma cell line SKMEL-19. PIM1-IN-1 has significant synergistic effect combined with different antitumoral agents in different tumor cell lines. PIM1-IN-1 (2.5, 5, or 10 μM, 24 hours) induces apoptosis in SKMEL19 cells.
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