I-OMe-Tyrphostin AG 538 (Synonyms: I-OMe-AG 538)
目录号: PL03487 纯度: ≥99%
CAS No. :1094048-77-7
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中文名称
I-OMe-Tyrphostin AG 538
英文名称
I-OMe-Tyrphostin AG 538
英文别名
2-[(3,4-dihydroxyphenyl)-oxomethyl]-3-(4-hydroxy-3-iodo-5-methoxyphenyl)-2-propenenitrile;HMS3372E12;2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile;Q27164335;(2E)-2-(3,4-Dihydroxybenzoyl)-3-(4-hydroxy-3-iod-5-methoxyphenyl)acrylonitril;(2E)-2-(3,4-Dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)acrylonitrile;(2E)-2-(3,4-Dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-méthoxyphényl)acrylonitrile;I-OMe-AG 538;I-OMe-Tyrphostin AG 538;α-Cyano-(3-methoxy-4-hydroxy-5-iodocinnamoyl)-(3',4'-dihydroxyphenyl)ketone;(E)-3-(4-hydroxy-3-iodo-5-methoxy-phenyl)-2-protocatechuoyl-acrylonitrile;Tyrphostin AG 538;α-Cyano-(3-methoxy-4-hydroxy-5-iodocinnamoyl)-(3′,4′-dihydroxyphenyl)ketone
Cas No.
1094048-77-7
分子式
C17H12InO5
分子量
437.19
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC 50  of 1 μM.
性状
Solid
IC50 & Target[1][2]
IC50: 1 μM (PI5P4Kα)
体外研究(In Vitro)
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) (0.1-1000 μM; 24 hours) is cytotoxic to PANC-1 cells in nutrient-deprived medium.
I-OMe-Tyrphostin AG 538 (0-3 μM; 1 hour) blocks phosphorylation of IGF-1R, Akt and Erk. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
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]. 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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (114.37 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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