DC661

DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis.

DC661 Chemical Structure

DC661 Chemical Structure

CAS: 1872387-43-3

Selleck's DC661 has been cited by 13 publications

Purity & Quality Control

Batch: S880801 Ethanol] 49 mg/mL] false] DMSO] 7 mg/mL] false] Water] Insoluble] false Purity: 99.7%
99.7

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Choose Selective Autophagy Inhibitors

Biological Activity

Description DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis.
Targets
Autophagy [1]
In vitro
In vitro

Treatment of melanoma cells with DC661 results in a more striking accumulation of the autophagic vesicle marker LC3B-II at lower concentrations compared with either Lys05 or HCQ, reflecting more pronounced accumulation of autophagic vesicles at concentrations between 0.1 and 10 μmol/L. All cells die at concentrations above 10 μmol/L for DC661 in contrast to Lys05 and HCQ. Compared with HCQ or Lys05, DC661 treatment induces a significantly more potent inhibition of autophagic flux in melanoma cells expressing the mCherry-eGFP-LC3B reporter, and significantly higher levels of free GFP in melanoma cells expressing GFP-LC3B. DC661 treatment resulted in significantly greater lysosomal deacidification compared with either HCQ or Lys05. The IC50 of DC661 in 72-hour MTT assays is 100-fold lower than that of HCQ across multiple cancer cell lines including colon and pancreas cancer cell lines. DC661 suppresses long-term clonogenic growth of melanoma cells more effectively and induces significantly more apoptosis than Lys05, HCQ, or combined BRAF and MEK inhibition in BRAF-mutant melanoma cells[1].

Cell Research Cell lines A375P cells
Concentrations 0.1, 0.3, 1, 3, 10 μM
Incubation Time 6 hours
Method

A375P cells are treated with doses of HCQ, Lys05, or DC661 for 6 hours before lysates are immunoblotted.

In Vivo
In vivo

Treatment with the reduced dose (3 mg/kg, i.p.) of DC661 in a HT29 xenograft results in a significant reduction in tumor volume and almost complete suppression of daily tumor growth rate compared with control mice without significantly affecting mouse weight[1].

Animal Research Animal Models HT29 colorectal xenograft
Dosages 3 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 552.58 Formula

C31H39Cl2N5

CAS No. 1872387-43-3 SDF --
Smiles CN(CCCCCCNC1=C2C=CC(=CC2=NC=C1)Cl)CCCCCCNC3=C4C=CC(=CC4=NC=C3)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Ethanol : 49 mg/mL

DMSO : 7 mg/mL ( (12.66 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Can you provide any information on how to formulate this compound for in vivo IP injection?

Answer:
Formula: 5% Stock solution (20 mg/ml)+40% PEG 300+5% Tween80+50% ddH2O, concentration:1mg/ml.

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