PIM1-IN-1 是一种有效、高度选择性的 PIM1/3 抑制剂，对 PIM1，PIM2 和 PIM3 的 IC50 值分别为 7，5530 和 70 nM。PIM1-IN-1 抑制 PIM 下游蛋白 BAD 的磷酸化，EC50 值为 262 nM，而对 FLT3 或 hERG 无作用。具有抗增殖、抗肿瘤作用。
货号:ajcx39268
CAS:1417630-95-5
分子式:C25H30N8O2
分子量：474.56
溶解度:DMSO : 45 mg/mL (94.82 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.

Protocol:

PIM1 7nM(IC50)

PIM3 70nM(IC50)

PIM2 5530nM(IC50)