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CAS No.: 1391426-24-6

Lys05 Catalog No. CSN22556

Synonyms: Lys05 (hydrochloride);Lys01;Lys01 3HCl

Lys05 is water soluble salt of Lys01. Lys05 shows potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Autophagy, the sequestration of organelles and proteins in autophagic vesicles (AVs) and degradation of this cargo through lysosomal fusion, allows tumor cells to survive metabolic and therapeutic stresses^[2]. Lys05, a dimeric chloroquine, is a new lysosomal autophagy inhibitor which more potently accumulates in the lysosome and blocks autophagy compared with hydroxychloroquine (HCQ)^[3]. C8161 xenografts matched for tumor size were treated with Lys05 (76 mg/kg; i.p.) for 48 h . Cells with intact nuclear and cytoplasmic membranes contained large AVs in Lys05-treated tumors. Meanwhile, significantly higher LC3II/LC3I levels were observed in Lys05-treated tumors compared with control- or HCQ-treated tumors, providing further evidence of in vivo autophagy inhibition. Mice bearing 1205Lu xenografts matched for tumor volume were treated with Lys05 (76 mg/kg; i.p.) and dosed for 3 d of daily treatment with 2 d off treatment. Lys05 treatment resulted in a 53% reduction in the average daily tumor growth rate compared with vehicle-treated controls. A significant six-fold accumulation of AV was observed at the end of 14 d of treatment in Lys05-treated tumors, compared with control group. Extensive tumor necrosis was observed in Lys05-treated tumors^[2].
动物研究
剂量
Mice: 10 mg/kg - 80 mg/kg^[2] (i.p.), 1 mg/kg - 20 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg - 80 mg/kg^[2] (i.p.), 1 mg/kg - 20 mg/kg^[3] (i.p.)
给药途径	i.p.

[2] McAfee Q, Zhang Z, Samanta A, Levi SM, Ma XH, Piao S, Lynch JP, Uehara T, Sepulveda AR, Davis LE, Winkler JD, Amaravadi RK. Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency. Proc Natl Acad Sci U S A. 2012 May 22;109(21):8253-8. doi: 10.1073/pnas.1118193109. Epub 2012 May 7. PMID: 22566612; PMCID: PMC3361415.
[3] Amaravadi RK, Winkler JD. Lys05: a new lysosomal autophagy inhibitor. Autophagy. 2012 Sep;8(9):1383-4. doi: 10.4161/auto.20958. Epub 2012 Aug 10. PMID: 22878685; PMCID: PMC3442884.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8190 mL
- 9.0950 mL
- 18.1901 mL
- 5 mM
- 0.3638 mL
- 1.8190 mL
- 3.6380 mL
- 10 mM
- 0.1819 mL
- 0.9095 mL
- 1.8190 mL

技术信息

CAS号

1391426-24-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H26Cl5N5

运输

蓝冰

分子量

549.75

别名

Lys05 (hydrochloride);Lys01;Lys01 3HCl;LYS-05 HCl;LYS-05;Lys01 (trihydrochloride);Lys01 HCl salt;Lys01 trihydrochloride

溶解度

DMSO	insoluble
Water	60.0 mg/mL (109.1 mM) warming

动物实验配方

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