化合物RG 13022 T3545

Product Introduction
Bioactivity


英文名: RG13022

描述: RG13022 (Tyrphostin RG13022) 是一种酪氨酸激酶抑制剂，抑制EGF 受体自身磷酸化的IC50值为4 μM。

细胞实验: 40 mM stock solutions of RG13022 is made in 100% DMSO and diluted with the culture medium before addition to the cells. MH-85 cells and HER 14 cells are plated in culture medium in the presence or absence of increasing concentrations of RG-13022 or RG-14620 for 10 days. At the end of culture, the cells are fixed with 4% (v/v) formaldehyde and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope[1].

体外活性: RG13022 suppresses EGF-stimulated cancer cell proliferation. In a cell-free reaction, RG13022 inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates (IC50: 4 μM). RG13022 inhibits colony formation (IC50: 1 μM) and DNA synthesis (IC50: 3 μM) by HER 14 cells (stimulated by 50 ng/mL EGF), in a dose-dependent manner. RG-13022 inhibits not only EGF-induced growth but also growth stimulated by insulin, insulin-like growth factor I, insulin-like growth factor II, or transforming growth factor alpha. RG-13022 also totally blocks estrogen-stimulated phosphorylation of the EGF receptor, as well as estrogen-induced cell proliferation, suggesting that functioning TK pathways are required for estrogen action.

体内活性: RG13022抑制裸鼠中的肿瘤生长，并延长了这些携带肿瘤裸鼠的寿命。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (187.76 mM)


关键字: HER1 | Inhibitor | RG13022 | EGFR | Tyrphostin RG-13022 | inhibit | ErbB-1 | Tyrphostin RG 13022 | RG-13022 | Epidermal growth factor receptor

相关产品: Erlotinib | WS3 | Neratinib | Nezutatug | PP2 | NRC-2694 | CGP52411 | Lifirafenib | Oritinib | (S)-Sunvozertinib

相关库: Angiogenesis related Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library | Covalent Inhibitor Library

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