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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 |
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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。
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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.
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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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N/A 生产厂家 全球有 8家供应商
N/A国内生产厂家
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上海波以尔化工有限公司
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Wuhan NCE Biomedical Co.,Ltd.
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1503
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上海皓元化学科技有限公司
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10011
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上海常丰生物医药科技有限公司
| +86 (21) 6172 7342 (21)6722 2512 +86 13611721451 | +86 (21) 6129 4107 | info@chainpharm.com / chainpharm@163.com / Offer Custom Synthesis | 中国 |
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上海惯承化工科技有限公司
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上海泽涵生物医药科技有限公司
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斯派螺(武汉)药物研发有限公司
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