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CA-5f Autophagy inhibitor

Cat.No.S5920

CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
CA-5f Autophagy inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 388.46

Quality Control

Batch: S592001 DMSO]78 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.57%
99.57

Chemical Information, Storage & Stability

Molecular Weight 388.46 Formula

C24H24N2O3

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1370032-19-1 -- Storage of Stock Solutions

Synonyms N/A Smiles CN1CC(=CC2=CC(=C(C=C2)OC)OC)C(=O)C(=CC3=CNC4=CC=CC=C43)C1

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (200.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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.
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Mechanism of Action

Targets/IC50/Ki
Autophagy [1]
In vitro
CA-5f neither impairs the hydrolytic function nor the quantity of lysosomes. Treatment of human umbilical vein endothelial cells (HUVECs) with this compound for 1 h suppresses the levels of cytoskeletal proteins and membrane traffic proteins. It exhibits strong cytotoxicity against A549 non-small cell lung cancer (NSCLC) cells, but low cytotoxicity to normal human umbilical vein endothelial cells (HUVECs), by increasing mitochondrial-derived reactive oxygen species (ROS) production. This chemical inhibits autophagic flux by blocking autophagosome-lysosome fusion instead of affecting the pH and hydrolytic function of lysosomes[1].
In vivo
CA-5f effectively suppresses the growth of A549 lung cancer xenograft as a single agent with an excellent tolerance in vivo. It inhibits autophagic flux, induced apoptosis, and does not affect the level of CTSB (cathepsin B) and CTSD (cathepsin D) in vivo[1].
References

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