产品
编 号:F139994
分子式:C16H14N2O2
分子量:266.29
产品类型
结构图
CAS No: 136831-48-6
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产品详情
生物活性:
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
体内研究:
RG13022 suppresses tumor growth in nude mice. RG13022 also increases the life span of these tumor-bearing nude mice.
体外研究:
RG13022 suppresses EGF-stimulated cancer cell proliferation. In a cell-free reaction RG13022 inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with an IC50 of 4 μM. RG13022 inhibits colony formation and DNA synthesis by HER 14 cells, which were stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50s are 1 and 3 μM for HER 14 colony formation and DNA synthesis, respectively. 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.