RG13022 (Tyrphostin RG13022) is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).

EGF:4 μM

RG13022 抑制 EGF 刺激的癌细胞增殖。在无细胞反应中，RG13022 抑制 EGF 受体在免疫沉淀物中的自磷酸化反应（IC50: 4 μM）。它还以剂量依赖性方式抑制 HER 14 细胞（由 50 ng/mL EGF 刺激）的集落形成（IC50: 1 μM）和 DNA 合成（IC50: 3 μM）。此外，RG-13022 不仅抑制 EGF 诱导的生长，还抑制由胰岛素、胰岛素样生长因子 I、胰岛素样生长因子 II 或转化生长因子阿尔法刺激的生长。RG-13022 还完全阻断了雌激素刺激的 EGF 受体磷酸化以及雌激素诱导的细胞增殖，这表明 TK（酪氨酸激酶）途径的功能是雌激素作用所必需的。

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。

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].