PIM1-IN-1
目录号: PL09853 纯度: ≥99%
CAS No. :1417630-95-5
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中文名称
PIM1-IN-1
英文名称
PIM1-IN-1
英文别名
PIM1-IN-1
Cas No.
1417630-95-5
分子式
C25H30N8O2
分子量
474.56
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC 50 s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC 50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.
性状
Solid
IC50 & Target[1][2]
PIM1 7 nM (IC50) PIM3 70 nM (IC50u
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.Apoptosis Analysis
体内研究(In Vivo)
PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 45 mg/mL (94.82 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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