货号:A646643 同义名: Tyrphostin RG13022
RG-13022 significantly inhibited EGF-stimulated autophosphorylation of its receptor in two breast cancer cell lines that have abundant, although not amplified, EGF receptor content (MDA-231 and T47D).RG-13022 suppressed not only EGF-stimulated cancer cell proliferation in vitro but also tumor growth in nude mice. RG-13022 also increased the life span of these tumor-bearing nude mice.
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描述 | Growth factor receptors with tyrosine kinase activity mediate paracrine and autocrine growth regulation of normal and malignant cells. The epidermal growth factor receptor (EGF-R) is a tyrosine kinase transmembrane protein that is overexpressed by many epithelial malignancies[1]. RG13022, a tyrosine kinase inhibitor, inhibits the autophosphorylation reaction of the EGF-R in immunoprecipitates with an IC50 of 4 μM. RG-13022 inhibits DNA synthesis and colony formation by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50s for RG-13022 are 3 μM and 1 μM for HER 14 DNA synthesis and HER 14 colony formation, respectively. RG-13022 also suppresses DNA synthesis and colony formation by EGF-stimulated MH-85 cells in a dose-dependent manner. The IC50s for RG-13022 on MH-85 cells are 1.5 μM and 7 μM for DNA synthesis and colony formation, respectively. Nude mice implanted with MH-85 tumors manifested profound hypercalcemia, cachexia, and leukocytosis as the tumor grew. RG-13022 (400 μg/mouse/day) significantly inhibits MH-85 tumor growth in Nude Mice. Because of slower tumor growth, MH-85 tumor-bearing animals receiving injections of RG-13022 show less cachexia and hypercalcemia, eat more food, and are more active than untreated MH-85 tumor-bearing animals. RG-13022 prolongs the life span of MH-85 tumor-bearing animals as a result of suppression of tumor growth. Moreover, administration of mAb108 i.p. (1 mg/mouse/day) at 1, 5, and 10 days after MH-85 inoculation of RG-13022 (400 μg/mouse/day) for 14 days profoundly inhibits MH-85 growth in nude mice[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.76mL 0.75mL 0.38mL |
18.78mL 3.76mL 1.88mL |
37.55mL 7.51mL 3.76mL |
CAS号 | 136831-48-6 |
分子式 | C16H14N2O2 |
分子量 | 266.295 |
别名 | Tyrphostin RG13022 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(394.3 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |