MEK/PI3K-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。

MEK/PI3K-IN-1 

MEK/PI3K-IN-1 (compound 6r) 是一种有效的 MEK/PI3K 抑制剂，其IC50 值分别为 124 nM (MEK1), 130 nM (PI3Kα), 和 236 nM (PI3Kδ)。MEK/PI3K-IN-1 抑制 pAKT 和 pERK1/2 水平。MEK/PI3K-IN-1 对肿瘤细胞具有抗增殖活性。

MEK/PI3K-IN-1

MEK/PI3K-IN-1 Chemical Structure

CAS No. : 2281803-28-7

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生物活性

MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines[1].

IC50 & Target

MEK1

124 ± 11 nM (IC50)

PI3Kα

130 ± 13 nM (IC50)

PI3Kδ

236 ± 29 nM (IC50)

PI3Kβ

1537 ± 188 nM (IC50)

PI3Kγ

2745 ± 485 nM (IC50)

分子量

913.63

Formula

C36H37F5IN9O6
CAS 号

2281803-28-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Dort ME, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996.

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