PIM1-IN-1 |
| Katalog-Nr.GC65278 |
PIM1-IN-1 ist ein potenter und hochselektiver PIM1/3-Inhibitor mit IC50-Werten von 7, 5530 und 70 nM fÜr PIM1, PIM2 bzw. PIM3 und hemmt die Phosphorylierung von BAD, einem nachgeschalteten Ziel von PIM, mit einem EC50 von 262 nM. PIM1-IN-1 zeigt keine offensichtliche Wirkung auf die FLT3- oder hERG-Bindung. Antiproliferative und Anti-Krebs-AktivitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1417630-95-5
Sample solution is provided at 25 µL, 10mM.
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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[1].
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[1]. PIM1-IN-1 (2.5, 5, or 10 µM, 24 hours) induces apoptosis in SKMEL19 cells[1].
PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice[1].
[1]. MartÍnez-GonzÁlez S, et al. Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. Eur J Med Chem. 2019 Feb 19;168:87-109.
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