Lys05

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Lys05（Lys01三盐酸盐，PS-1001）是Lys01的水溶性盐，是一种比羟氯喹（HCQ）强10倍的溶酶体自噬抑制剂；在MTT测定中显示1205Lu、c8161、LN229和HT-29细胞系的IC50值为3.6、3.8、6和7.9 uM。

Lys05 (Lys01 trihydrochloride, PS-1001)?is the water-soluble salt of Lys01, is a 10-fold more potent lysosomal autophagy inhibitor than hydroxychloroquine (HCQ); shows IC50 values of 3.6, 3.8, 6 and 7.9 uM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay;?more potently accumulates within and deacidifies the lysosome, resulting in impaired autophagy and tumor growth; enhances sunitinib-mediated suppression of clear cell ovarian carcinoma (CCOC) cell viability.

Lys01, is a 10-fold more potent autophagy inhibitor than HCQ. Compared with HCQ, Lys05, a water-soluble salt of Lys01, more potently accumulates within and deacidifies the lysosome. Lys01 and Lys05 produce equivalent dose-dependent increases in the LC3II/LC3I ratio, accumulation of the autophagy cargo protein p62, and identical IC50 values in the MTT assay.

With this high-dose, short-term treatment, no mice die, but after 2 d of dosing, mice treated with Lys05 76 mg/kg i.p. are observed to have arched backs and lethargy. Morphologically, EM show that cells with intact nuclear and cytoplasmic membranes contain large AVs in Lys05-treated tumors. Tumor growth is significantly impaired in Lys05-treated tumors compared with controls. Lys05 treatment results in a 53% reduction in the average daily tumor growth rate compared with vehicle-treated controls. A significant three- and six-fold accumulation of AV is observed at the end of 14 d of treatment in HCQ- and Lys05-treated tumors, respectively, compared with control-treated tumors.

Lys-05 | Lys 05 | Lys01 trihydrochloride | PS-1001

Autophagy

Autophagy

lysosomalautophagy(1205Lu)|lysosomalautophagy(c8161)|lysosomalautophagy(HT-29)|lysosomalautophagy(LN229)

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1391426-24-6

549.75

C23H26Cl5N5

>98% (HPLC)

DMSO: 6.4 mg/mL, Need Ultrasonic; Water: 3 mg/mL (5.5 mM); Ethanol: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CN(CCNC1=CC=NC2=CC(Cl)=CC=C12)CCNC3=CC=NC4=CC(Cl)=CC=C34.[H]Cl.[H]Cl.[H]Cl

N2-(7-Chloro-4-quinolinyl)-N1-[2-[(7-chloro-4-quinolinyl)amino]ethyl]-N1-methyl-1,2-ethanediamine trihydrochloride

(-20℃)

With Ice Pack

≥ 2 years