685898-44-6
中文名稱
(S)-4-(2-氨基-2-羧乙基)-N,N-雙(2-氯乙基)環(huán)己-1,3-二苯胺氧化物二鹽酸鹽
英文名稱
L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
CAS
685898-44-6
分子式
C13H20Cl4N2O3
分子量
394.13
MOL 文件
685898-44-6.mol
更新日期
2024/09/23 15:45:04
685898-44-6 結(jié)構(gòu)式
基本信息
中文別名
(S)-4-(2-氨基-2-羧乙基)-N,N-雙(2-氯乙基)環(huán)己-1,3-二苯胺氧化物二鹽酸鹽 英文別名
CS-1467PX-478 HCl
PX478 2HCl
PX 478 DISCONTINUED
PX-478 dihydrochloride
4-[Bis(2-chloroethyl)oxidoamino]-L-phenylalanine dihydrochloride
4-[bis(2-chloroethyl)oxidoamino]-L-phenylalanine,hydrochloride (1:2)
L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1
Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
所屬類別
生物化工：HIF 抑制劑物理化學(xué)性質(zhì)
儲存條件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度≥19.7 mg/mL in DMSO; ≥50 mg/mL in H2O; ≥8.42 mg/mL in EtOH
形態(tài)粉末
顏色Off-white to yellow
CAS 數(shù)據(jù)庫685898-44-6
常見問題列表
生物活性
PX-478 2HCl是一種具有口服活性的選擇性hypoxia-inducible factor-1α (HIF-1α)抑制劑。Phase 1。體外研究
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.體內(nèi)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.生物活性
PX-478 2HCl 是一種具有口服活性的選擇性hypoxia-inducible factor-1α (HIF-1α)抑制劑。PX-478 2HCl可誘導(dǎo)凋亡并具有抗腫瘤的活性。Phase 1。靶點(diǎn)
| Target | Value |
| HIF-1α |
體外研究
PX-478降低缺氧和常氧環(huán)境下各種細(xì)胞系中HIF-1α蛋白水平和HIF-1反式激活，并且對蛋白質(zhì)的翻譯具有更顯著的作用，比如缺氧環(huán)境下的 HIF-1α。 PX-478也能夠增強(qiáng)前列腺癌PC3細(xì)胞的放射敏感性。
體內(nèi)研究
在HT-29人結(jié)腸癌異種移植物中，PX-478抑制HIF-1α的水平，并抑制HIF-1靶點(diǎn)基因的表達(dá)，包括血管內(nèi)皮生長因子和葡萄糖轉(zhuǎn)運(yùn)體-1。此外，PX-478 (100 或120 mg/kg i.p.)也表現(xiàn)出抗腫瘤活性，包括治愈幾種建立的與HIF-1α水平相關(guān)的人腫瘤異種移植物。在高脂飲食小鼠體內(nèi)，PX-478減少它們脂肪組織中的纖維化病變和炎癥浸潤。(S)-4-(2-氨基-2-羧乙基)-N,N-雙(2-氯乙基)環(huán)己-1,3-二苯胺氧化物二鹽酸鹽價格(試劑級)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2024/11/08 | S7612 | PX-478 2HCl | 685898-44-6 | 1mg*5 | 1203.93元 |
| 2024/11/08 | S7612 | (S)-4-(2-氨基-2-羧乙基)-N,N-雙(2-氯乙基)環(huán)己-1,3-二苯胺氧化物二鹽酸鹽 PX-478 2HCl | 685898-44-6 | 25mg | 3886.42元 |
| 2024/11/08 | S7612 | (S)-4-(2-氨基-2-羧乙基)-N,N-雙(2-氯乙基)環(huán)己-1,3-二苯胺氧化物二鹽酸鹽 PX-478 2HCl | 685898-44-6 | 100mg | 8177.68元 |