Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 285 | 现货 | ||
2 mg | ¥ 423 | 现货 | ||
5 mg | ¥ 727 | 现货 | ||
10 mg | ¥ 1,130 | 现货 | ||
25 mg | ¥ 2,220 | 现货 | ||
50 mg | ¥ 3,290 | 现货 | ||
100 mg | ¥ 4,680 | 现货 | ||
500 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 939 | 现货 |
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. |
靶点活性 | HT29 cells:7.9 μM, LN229:6μM, 1205Lu:3.6μM, C8161 cells:3.8μM |
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]. |
别名 | Lys01 trihydrochloride |
分子量 | 549.75 |
分子式 | C23H26Cl5N5 |
CAS No. | 1391426-24-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 3 mg/mL(5.5 mM)
DMSO: 5.5 mg/mL (10 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 1.819 mL | 9.095 mL | 18.1901 mL | 45.4752 mL |
5 mM | 0.3638 mL | 1.819 mL | 3.638 mL | 9.095 mL | |
DMSO | 10 mM | 0.1819 mL | 0.9095 mL | 1.819 mL | 4.5475 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Lys05 1391426-24-6 Autophagy lysosomal autophagy Inhibitor Lys-05 Lys01 Trihydrochloride inhibit Lys01 trihydrochloride Lys 05 Lys01 inhibitor