143851-98-3

• 常用中文名：依克立达盐酸盐
• 常用英文名：Elacridar hydrochloride
• CAS号：143851-98-3
• 分子式：C₃₄H₃₄ClN₃O₅
• 分子量：600.10400
• 相关类别： 信号通路 跨膜转运 P-糖蛋白
• 发布时间：2018-03-10 08:00:00
• 更新时间：2026-07-11 19:37:47
• Elacridar(GF120918; GW0918)盐酸盐是P-糖蛋白抑制剂,在体内外实验中常作为工具化合物。

名称

• 中文名: 依克立达盐酸盐
• 英文名: N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide,hydrochloride
• 中文别名: 盐酸盐依克立达; ELACRID盐酸盐; N-(4-(2-(6,7-二甲氧基-3,4-二氢异喹啉-2(1H)-基)乙基)苯基)-5-甲氧基-9-氧代-9,10-二氢吖啶-4-甲酰胺 盐酸盐
• 英文别名: N-(4-(2-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-5-methoxy-9-oxo-9,10-dihy; Elacrid(hydrochloride); EOS-62093; ElacridHCl (GF120918A); N-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-5-methoxy-9-oxo-9,10-dihydroacridine-4-cboxamidehydrochloride; UNII-NX2BHH1A5B; 4-Acridinecboxamide, N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-, hydrochloride (1:1); Elacridar (hydrochloride); ElacridHCl; N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-cboxamide,hydrochloride; ElacridHC1; N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecboxamide monohydrochloride; 1-{2-cbaMoyl-5-[2-(6,7-diMethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]phenyl}-5-Methoxy-9-oxo-9,10-dihydroacridine-4-cboxylic acid hydrochloride; Elacridar hydrochloride (USAN); GW 0918 N-[4-[2-(3,4-Dihydro-6,7-diMethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-Methoxy-9-oxo-4-acridinecboxaMide, (HCl salt); GF 120918A; GF120918A; GF-120918A; Elacridar HCl; ElacridHCl //BP; N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecboxamide hydrochloride

物化性质

• 沸点: 701.6ºC at 760 mmHg
• 分子式: C₃₄H₃₄ClN₃O₅
• 分子量: 600.10400
• 闪点: 378.1ºC
• 精确质量: 599.21900
• PSA: 92.89000
• LogP: 6.37310
• 蒸汽压: 1.57E-19mmHg at 25°C
• 储存条件: 2-8℃

生物活性

• 描述: Elacridar(GF120918; GW0918)盐酸盐是P-糖蛋白抑制剂,在体内外实验中常作为工具化合物。
• 相关类别:
  信号通路 >> 跨膜转运 >> P-糖蛋白
  研究领域 >> 癌症
• 参考文献:

  [1]. Sane R, Mittapalli RK, Elmquist WF. Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci. 2013 Jan 18.

  [2]. Bankstahl JP, Bankstahl M, Romermann K, et al. Tariquidar and Elacridar Are Dose-Dependently Transported by P-Glycoprotein and Bcrp at the Blood-Brain Barrier: A Small-Animal PET and In-Vitro Study. Drug Metab Dispos. 2013 Jan 10.

  [3]. Sane R, Agarwal S, Elmquist WF. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.

  [4]. Tang SC, Lagas JS, Lankheet NA, et al. Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration. Int J Cancer. 2012 Jan 1;130(1):223-33. doi: 10.1002/ijc.26000.

  [5]. Kuppens IE, Witteveen EO, Jewell RC, et al. A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res. 2007 Jun 1;13(11):3276-85.

  [6]. Hong Xiao, et al. Polymeric nanovesicle as simultaneous delivery platform with Doxorubicin conjugation and Elacridar encapsulation for enhanced treatment of multidrug-resistant breast cancer. J. Mater. Chem. B. 2018 Oct.

安全

• 海关编码: 2934999090

海关

海关编码	2934999090
中文概述	2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%