Name | DC661 |
Synonyms | DC661 DC-661 DC 661 N'-(7-Chloro-4-quinolinyl)-N-{6-[(7-chloro-4-quinolinyl)amino]hexyl}-N-methyl-1,6-hexanediamine 1,6-Hexanediamine, N6-(7-chloro-4-quinolinyl)-N1-[6-[(7-chloro-4-quinolinyl)amino]hexyl]-N1-methyl- |
CAS | 1872387-43-3 |
Molecular Formula | C31H39Cl2N5 |
Molar Mass | 552.58 |
Density | 1.210±0.06 g/cm3(Predicted) |
Boling Point | 726.8±60.0 °C(Predicted) |
Solubility | Soluble in DMSO |
pKa | 9.77±0.50(Predicted) |
Storage Condition | -20℃ |
Use | DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor. DC661 inhibits autophagy. DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). |
Target | PPT1, autophagy |
In vitro study | Treatment of melanoma cells with DC661 caused an accumulation of the autophagic vesicle marker LC3B-II, an accumulation effect that was more pronounced than Lys05 or HCQ, and at lower concentrations. When the concentration of DC661 was greater than 10 μm, all cells died. Compared with HCQ and Lys05, DC661 was more effective in suppressing autophagic flux in melanoma cells expressing mCherry-eGFP-LC3B reporter gene, and in melanoma cells expressing GFP-LC3B reporter gene, higher levels of free GFP were expressed. DC661 can cause a more significant lysosomal deacidification effect. In a variety of cancer cell lines (including colon cancer cells and pancreatic cancer cells), The IC50 of DC661 was 100 times lower than that of HCQ after 72 hours of drug incubation. In BRAF-mutated melanoma cell lines, DC661 was more effective in inhibiting the clonal growth of long-term melanoma cells and inducing more apoptosis than Lys05, HCQ, or BRAF/MEK dual inhibition conditions. |
In vivo study | In the HT29 xenograft model, intraperitoneal injection of 3 mg/kg DC661 resulted in a significant reduction in tumor volume, and the daily tumor growth rate was completely suppressed by several times. But it did not affect the body weight of mice. |
Reference Show more | [1]. Rebecca VW, et al. PPT1 Promotes Tumor Growth and Is the Molecular Target of Chloroquine Derivatives in Cancer. ancer Discov. 2019 Feb;9(2):220-229. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.81 ml | 9.048 ml | 18.097 ml |
5 mM | 0.362 ml | 1.81 ml | 3.619 ml |
10 mM | 0.181 ml | 0.905 ml | 1.81 ml |
5 mM | 0.036 ml | 0.181 ml | 0.362 ml |