I-OMe-Tyrphostin AG 538

• 常用名: I-OMe-Tyrphostin AG 538
• 英文名: I-OMe-Tyrphostin AG 538
• CAS号: 1094048-77-7
• 分子量: 437.19
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₇H₁₂INO₅
• 熔点: N/A
• 闪点: N/A

I-OMe-Tyrphostin AG 538用途

I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) 是 IGF-1R 激酶的特异性抑制剂。I-OMe-Tyrphostin AG 538 抑制 IGF-1R 介导的信号传导,并优先对营养缺乏的 PANC1 细胞产生细胞毒性。I-OMe-Tyrphostin AG 538 是具有 ATP 竞争性的 PI5P4Kα抑制剂,IC50 为 1 μM。

I-OMe-Tyrphostin AG 538名称

• 英文名: I-OMe-Tyrphostin AG 538

I-OMe-Tyrphostin AG 538生物活性

• 描述: I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) 是 IGF-1R 激酶的特异性抑制剂。I-OMe-Tyrphostin AG 538 抑制 IGF-1R 介导的信号传导,并优先对营养缺乏的 PANC1 细胞产生细胞毒性。I-OMe-Tyrphostin AG 538 是具有 ATP 竞争性的 PI5P4Kα抑制剂,IC50 为 1 μM。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 蛋白酪氨酸激酶 >> IGF-1R
  研究领域 >> 代谢疾病
• 靶点实验:

  IC50: 1 µM (PI5P4Kα)[1]

• 体外研究: I-OMe-Tyrphostin AG 538(I-OMe-AG 538)(0.1-1000μM；24小时)对营养缺乏培养基中的PANC-1细胞具有细胞毒性[1]。I-OMe-Tyrphostin AG 538(0-3μM；1小时)阻断IGF-1R、Akt和Erk的磷酸化[1]。细胞活力测定[1]细胞系：PANC-1细胞浓度：0.1,1,10,1000μM培养时间：24小时结果：在营养缺乏的培养基中对PANC-1细胞有细胞毒性。Western Blot分析[1]细胞系：PANC-1细胞(50ng/ml IGF-1刺激10min)浓度：0.03,0.3,3μM孵育时间：1h结果：IGF-1R、Akt和Erk磷酸化受阻。
• 参考文献:

  [1]. Davis MI, et al. A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation. PLoS One. 2013;8(1):e54127.

  [2]. Momose I, et al. Inhibitors of insulin-like growth factor-1 receptor tyrosine kinase are preferentially cytotoxic to nutrient-deprived pancreatic cancer cells. Biochem Biophys Res Commun. 2009 Feb 27;380(1):171-6.

I-OMe-Tyrphostin AG 538物理化学性质

• 分子式: C₁₇H₁₂INO₅
• 分子量: 437.19
• InChIKey: HSRMHXWCTRFVHK-NYYWCZLTSA-N
• SMILES: COc1cc(C=C(C#N)C(=O)c2ccc(O)c(O)c2)cc(I)c1O
• 储存条件: 2-8°C，干燥，密封

I-OMe-Tyrphostin AG 538安全信息

• 危害码 (欧洲): Xi

I-OMe-Tyrphostin AG 538靶点实验

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