RG14620是一种EGFR抑制剂,IC50值为3 μM。
产品描述
RG14620 is an epidermal growth factor receptor (EGFR) inhibitor.
体外活性
RG-14620 inhibits colony formation and DNA synthesis by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50s for RG-14620 are 3 μM for HER 14 colony formation and 1 pM for HER 14 DNA synthesis[1]. RG-14620 also suppresses colony formation and DNA synthesis by EGF-stimulated MH-85 cells in a dose-dependent manner. The IC50s for RG-14620 on MH-85 cells are 4 μM for colony formation and 1.25 μM for DNA synthesis[1].
体内活性
RG-14620, at a dose of 200 μg/mouse/day inhibits MH-85 tumor growth in nude mice. Mice show less cachexia and hypercalcemia, eat more food, and are more active than untreated MH-85 tumor-bearing animals[1].
细胞实验
RG14620 is dissolved in 100% DMSO and diluted with the culture medium before addition to the cells. MH-85 and HER 14 cells are cultured in the 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 in calcium-magnesium-free phosphate-buffered saline for 15 min at room temperature and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope[1].
Cas No.
136831-49-7
分子式
C14H8Cl2N2
分子量
275.13
别名
RG 14620;Tyrphostin RG14620
储存和溶解度
DMSO:26 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years