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Lys05

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Chemical Structure| 1391426-24-6 同义名 : Lys01 trihydrochloride;Lys01;Lys05 (hydrochloride)
CAS号 : 1391426-24-6
货号 : A209517
分子式 : C23H26Cl5N5
纯度 : 99%+
分子量 : 549.751
MDL号 : MFCD28963913
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(9.1 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 6 mg/mL(10.91 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Autophagy
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.82mL

0.36mL

0.18mL

9.10mL

1.82mL

0.91mL

18.19mL

3.64mL

1.82mL
参考文献

[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.