您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Lys05
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Lys05
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lys05图片
CAS NO:1391426-24-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Lys01 trihydrochloride
产品介绍
Lys05 是一种有效的水溶性溶酶体自噬抑制剂,具有抗肿瘤活性。在MTT试验中,对1205Lu、c8161、LN229 和HT-29细胞系的IC50值分别为3.6、3.8、6 和7.9 μM。

产品描述

Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models compared with HCQ. Lys05 is therefore a new lysosomal autophagy inhibitor that has potential to be developed further into a drug for cancer and other medical applications.

体外活性

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 lys01 trihydrochloride 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[1].

体内活性

With this high-dose, short-term treatment, no mice die, but after 2 d of dosing, mice treated with lys01 trihydrochloride 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 lys01 trihydrochloride-treated tumors. Tumor growth is significantly impaired in lys01 trihydrochloride-treated tumors compared with controls. Lys01 trihydrochloride 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 lys01 trihydrochloride-treated tumors, respectively, compared with control-treated tumors[1].

细胞实验

1205Lu, c8161, LN229 and HT-29 cells are treated with lys01 trihydrochloride (0, 0.01, 0.1, 1, and 10 μM) or Lys01 (0, 0.01, 0.1, 1, and 10 μM) in five replicates for 72 h. The Acid Phsophatase Assay kit is used for the MTT assay[1].

Cas No.

1391426-24-6

分子式

C23H26Cl5N5

分子量

549.75

别名

Lys01 trihydrochloride

储存和溶解度

Ethanol:<1 mgml
H2O:3 mg/mL(5.5 mM)
DMSO:6.4 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years