产品信息
抗原名称
HIF-1α
商品描述
PX-478 is HIF-1alpha inhibitor, is also an orally active small molecule with potential antineoplastic activity. PX-478 has excellent activity against established human tumor xenografts, providing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. PX-478 is a highly water soluble molecule, with good i.v., i.p. and p.o. antitumor activity.
分子量
394.12
纯度
>98%
可溶性
DMSO 78 mg/mL (197.9 mM)
Water 78 mg/mL (197.9 mM)
Ethanol 78 mg/mL (197.9 mM)
Water 78 mg/mL (197.9 mM)
Ethanol 78 mg/mL (197.9 mM)
In vitro(体外研究)
PX-478 lowers HIF-1α protein levels and HIF-1 transactivation in hypoxia and in normoxia in a variety of cancer cell lines, but has a more pronounced effect on translation of proteins, such as HIF-1α in hypoxia. PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells.
In vivo(体内研究)
In HT-29 human colon cancer xenografts, PX-478 suppresses HIF-1alpha levels and inhibits the expression of HIF-1 target genes including vascular endothelial growth factor and the glucose transporter-1. In addition, PX-478 (100 or 120 mg/kg i.p.) also shows antitumor activity including cures against several established human tumor xenografts that is related to the levels of HIF-1α. In high-fat-diet mice, PX-478 causes reduced fibrosis and fewer inflammatory infiltrates in their adipose tissues.
背景
分子式
C13H20Cl4N2O3
CAS号
685898-44-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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