PIM1-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PIM1-IN-1  纯度: 99.51%

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。

PIM1-IN-1

PIM1-IN-1 Chemical Structure

CAS No. : 1417630-95-5

规格 价格 是否有货 数量
5 mg ￥3800 In-stock
10 mg ￥6000 In-stock
25 mg ￥11500 In-stock
50 mg   询价  
100 mg   询价  

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PIM1-IN-1 相关产品

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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[1].

IC50 & Target[1]

PIM1

7 nM (IC50)

PIM3

70 nM (IC50)

PIM2

5530 nM (IC50)

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[1].
PIM1-IN-1 (2.5, 5, or 10 µM, 24 hours) induces apoptosis in SKMEL19 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: SKMEL19 cells
Concentration: 2.5, 5, or 10 µM
Incubation Time: 24 hours
Result: Regulated cell cycle, induced cell apopsis in SKMEL19 cells.

体内研究
(In Vivo)

PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

474.56

Formula

C25H30N8O2
CAS 号

1417630-95-5
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 45 mg/mL (94.82 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1072 mL 10.5361 mL 21.0722 mL
5 mM 0.4214 mL 2.1072 mL 4.2144 mL
10 mM 0.2107 mL 1.0536 mL 2.1072 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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