aladdin 阿拉丁 P408756 PX-478 2HCl 685898-44-6 10mM in DMSO

中文名：PX-478 2HCl

英文名：PX-478 2HCl

英文别名：4-[bis(2-chloroethyl)oxidoamino]-L-phenylalanine,hydrochloride (1:2)

纯度：10mM in DMSO

货号：P408756

包装：1ml

Cas号：685898-44-6

存储温度：-80℃储存

产品介绍：

Information

PX-478 2HCl PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
In vitro

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

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.
Cell Data

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