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生物活性 体外研究 体内研究

CAS号:685898-44-6
英文名称:L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
英文同义词:PX-478 HCl;PX478 2HCl;PX-478 dihydrochloride;4-[bis(2-chloroethyl)oxidoamino]-L-phenylalanine,hydrochloride (1:2);L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
中文名称:N/A
中文同义词:
CBNumber:CB02628046
分子式:C13H20Cl4N2O3
分子量:0
MOL File:Mol file
N/A化学性质
安全信息

N/A 性质、用途与生产工艺

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.
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685898-44-6, N/A 相关搜索:
艾乐替尼(alectinib,CH5424802) 2-甲氧雌二醇 BGJ398 (NVP-BGJ398) BAY87-2243 苹果酸舒尼替尼 盐酸多柔比星
C13H20Cl4N2O3 685898-44-6 PX-478 HCl 4-[bis(2-chloroethyl)oxidoamino]-L-phenylalanine,hydrochloride (1:2) PX478 2HCl PX-478 dihydrochloride L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
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