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Purity: ≥98%
CA-5f (CA5f) is a novel and potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion with anti-tumor activity. It has potent anti-tumor effect against non-small cell lung cancer. CA-5f neither impaired the hydrolytic function nor the quantity of lysosomes. Use of an isobaric tag for relative and absolute quantitation (iTRAQ)-based proteomic screen in combination with bioinformatics analysis suggested that treatment of human umbilical vein endothelial cells (HUVECs) with CA-5f for 1 h suppressed the levels of cytoskeletal proteins and membrane traffic proteins. Subsequent studies showed that CA-5f exhibited 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.
Targets |
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ln Vitro |
In A549 cells and HUVEC, CA-5f (0-40 μM, 6 hours) elevates the levels of SQSTM1 protein and LC3B-II (an autophagy monitoring marker) in a concentration- and time-dependent manner [1]. A549 cells and HUVECs treated with CA-5f (20 μM, 6 hours) or in combination with Bafilomycin A1 (100 nM) or Chloroquine (30 μM) do not exhibit autophagosome degradation [1]. Neither the number of lysosomes nor the hydrolytic function are impacted by CA-5f (20 μM) [1]. CA-5f (20 μM, 96 hours) is less harmful to normal HUVECs and suppresses the development of A549 cells [1].
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ln Vivo |
In nude mice containing A549 lung cancer cells, CA-5f (40 mg/kg, intraperitoneal injection, once every two days, up to 30 days) is well tolerated and can successfully stop tumor growth [1]. Using A549 lung cancer cells, CA-5f (40 mg/kg, ip) suppresses autophagy flux and causes apoptosis in nude mice [1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: A549, HUVECs Tested Concentrations: 20 μM Incubation Duration: 96 hrs (hours) Experimental Results: demonstrated more cytotoxicity against A549 cells compared with normal HUVECs. Western Blot Analysis[1] Cell Types: A549 cells and HUVECs Tested Concentrations: 0 -40 μM Incubation Duration: 6 hrs (hours) Experimental Results: Elevated LC3B-II (a marker to monitor autophagy) and SQSTM1 protein levels in a concentration- and time-dependent manner. |
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Animal Protocol |
Animal/Disease Models: Nude mice bearing A549 lung cancer cells[1]
Doses: 40 mg/kg Route of Administration: Injected via caudal vein, every 2 days for up to 30 days Experimental Results: Dramatically suppressed tumor volume and weight in mice, increased the number of apoptotic cells in mice. |
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References |
[1]. Zhang L, et al. Identification of compound CA-5f as a novel late-stage autophagy inhibitor with potent anti-tumor effect against non-small cell lung cancer. Autophagy. 2019 Mar;15(3):391-406.
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Molecular Formula |
C₂₄H₂₄N₂O₃
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Molecular Weight |
388.46
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CAS # |
1370032-19-1
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SMILES |
O=C(/C(CN(C)C/1)=C/C2=CNC3=C2C=CC=C3)C1=C\C4=CC=C(OC)C(OC)=C4
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Chemical Name |
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (5.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5743 mL | 12.8713 mL | 25.7427 mL | |
5 mM | 0.5149 mL | 2.5743 mL | 5.1485 mL | |
10 mM | 0.2574 mL | 1.2871 mL | 2.5743 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.