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发布者：信康 浏览次数：
产品名称:N/ACAS:685898-44-6别名：英文名：L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
[] - 生物活性PX-478 2HCl是一种具有口服活性的选择性hypoxia-inducible factor-1α (HIF-1α)抑制剂。Phase 1。
- 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.
- 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.
