中文同义词:
酪氨酸磷酸化抑制剂RG14620;EGFR抑制剂(RG14620);TYRPHOSTIN RG 14620 酪氨酸磷酸化抑制剂RG14620;酪氨酸磷酸化抑制剂RG14620;化合物RG 14620
英文同义词:
RG-14620;TYRPHOSTIN RG 14620;2-(3,5-DICHLOROPHENYL)-1-(3-PYRIDINYL)ACRYLONITRILE;2-(3-Pyridinyl)-3-(3,5-dichlorophenyl)propenenitrile;RG 14620,, 136831-49-7;3-Pyridineacetonitrile,a-[(3,5-dichlorophenyl)methylene]-;RG 14620; RG-14620; TYRPHOSTIN RG14620;RG14620, >98%
沸点
418.2±45.0 °C(Predicted)
密度
1.355±0.06 g/cm3(Predicted)
酸度系数(pKa)
2.97±0.12(Predicted)
生物活性
RG14620 (Tyrphostin RG14620)是一种EGFR抑制剂,可直接抑制ABCG2/BCRP的传送功能。
靶点
Target Value
EGFR
()
ABCG2
()
体外研究
RG14620 inhibits colony formation (IC 50 =3 μM) and DNA synthesis (IC 50 =1 μM) by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. RG14620 also suppresses colony formation(IC 50 =4 μM) and DNA synthesis (IC 50 =1.25 μM) by EGF-stimulated MH-85 cells in a dose-dependent manner. The growth-inhibitory effect of RG14620 irreversible.
体内研究
RG14620, at a dose of 200 g/mouse/day inhibits H-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.