PIM1-IN-1 |
| Catalog No.GC65278 |
PIM1-IN-1은 PIM1, PIM2 및 PIM3에 대해 각각 IC50이 7, 5530 및 70nM인 강력하고 고도로 선택적인 PIM1/3 억제제이며 EC50으로 PIM의 다운스트림 표적인 BAD의 인산화를 억제합니다. 262nM의. PIM1-IN-1은 FLT3 또는 hERG 결합에 명백한 효과를 나타내지 않습니다. 항증식 및 항암 활성.
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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