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ChemicalBook--->CAS DataBase List--->1872387-43-3

1872387-43-3

        1872387-43-3 Structure

        1872387-43-3 Structure
        IdentificationBack Directory
        [Name]

        DC661
        [CAS]

        1872387-43-3
        [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-
        [Molecular Formula]

        C31H39Cl2N5
        [MDL Number]

        MFCD31812586
        [MOL File]

        1872387-43-3.mol
        [Molecular Weight]

        552.58
        Chemical PropertiesBack Directory
        [Boiling point ]

        726.8±60.0 °C(Predicted)
        [density ]

        1.210±0.06 g/cm3(Predicted)
        [storage temp. ]

        Store at -20°C
        [solubility ]

        DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:4): 0.20 mg/ml; DMSO: 25 mg/ml; Ethanol: 15 mg/ml
        [form ]

        A solid
        [pka]

        9.77±0.50(Predicted)
        [color ]

        White to yellow
        Hazard InformationBack Directory
        [Uses]

        DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity[1].
        [Biological Activity]

        DC661 is able to deacidify lysosomes and significantly inhibit autophagy, which is more effective than hydroxychloroquine (HCQ). It induces apoptosis.
        [in vitro]

        Treatment of melanoma cells with DC661 induced the accumulation of the autophagic vacuole marker LC3B-II, which was more pronounced and lower than that of Lys05 or HCQ. At concentrations of it greater than 10 μM, all cells died. Compared with HCQ and Lys05, DC661 inhibited autophagic flux more significantly in melanoma cells expressing the mCherry-eGFP-LC3B reporter gene; in melanoma cells expressing the GFP-LC3B reporter gene, the expression level was higher of free GFP levels. It can cause a more pronounced lysosomal deacidification effect. In a variety of cancer cell lines, including colon and pancreatic cancer cells, the IC50 of DC661 was 100-fold lower than that of HCQ as measured by MTT assay after 72 hours of drug incubation. In BRAF-mutated melanoma cell lines, it inhibited the clonal growth of long-term melanoma cells more effectively and induced more apoptosis than Lys05, HCQ or BRAF/MEK dual inhibition conditions.

        [in vivo]

        In the HT29 xenograft model, intraperitoneal injection of 3 mg/kg DC661 caused a significant decrease in tumor volume, and the daily tumor growth rate was completely inhibited several times. but did not affect the body weight of mice.

        [target]

        TargetValue
        Autophagy
        ()
        [storage]

        Store at -20°C
        [References]

        [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. DOI:10.1158/2159-8290.CD-18-0706
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