| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models compared with HCQ. Lys05 is therefore a new lysosomal autophagy inhibitor that has potential to be developed further into a drug for cancer and other medical applications.
| ln Vitro |
The autophagy inhibitor Lys01 is ten times more effective than HCQ. Compared to HCQ, Lys01's water-soluble salt, Lys05, accumulates and deacidifies lysosomes more effectively. In MTT experiments, Lys01 and Lys05 result in the same IC50 values, accumulation of the autophagy cargo protein p62, and dose-dependent increases in the LC3II/LC3I ratio [1].
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| ln Vivo |
No mice died from this high-dose, short-term treatment; nevertheless, mice treated with Lys05 76 mg/kg ip showed signs of lethargy and bent backs two days after dosing. Large AVs were found morphologically in cells with intact nuclear and cytoplasmic membranes in Lys05-treated tumors, as demonstrated by electron microscopy. When compared to controls, Lys05-treated tumors showed a substantial reduction in tumor growth. When compared to vehicle-treated controls, the mean daily tumor growth rate decreased by 53% after receiving Lys05 therapy. When HCQ- and Lys05-treated tumors were compared to control-treated tumors at the end of their 14-day therapy, there was a noticeable three-fold and six-fold increase in AV accumulation [1].
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| References |
[1]. McAfee Q, et al. Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency. Proc Natl Acad Sci U S A. 2012 May 22;109(21):8253-8
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| Molecular Formula |
C23H26CL5N5
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|---|---|
| Molecular Weight |
549.75
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| Exact Mass |
547.063
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| CAS # |
1391426-24-6
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| Related CAS # |
Lys01;1391426-22-4
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| PubChem CID |
70673566
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| Appearance |
Light brown to gray solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
480
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=CC=C(NCCN(CCNC2C3C=CC(=CC=3N=CC=2)Cl)C)C2C=CC(=CC1=2)Cl.Cl.Cl.Cl
|
| InChi Key |
N2-(7-Chloro-4-quinolinyl)-N1-[2-[(7-chloro-4-quinolinyl)amino]ethyl]-N1-methyl-1,2-ethanediamine trihydrochloride
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| InChi Code |
JTUYDBHQGOZPQQ-UHFFFAOYSA-N
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| Chemical Name |
LYS-05 HCl LYS05 LYS-05 Lys01 (trihydrochloride) Lys01 HCl salt.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~25 mg/mL (~45.48 mM)
H2O : ~6.4 mg/mL (~11.64 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (13.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 75.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 4.17 mg/mL (7.59 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 41.7 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 | 1.8190 mL | 9.0950 mL | 18.1901 mL | |
| 5 mM | 0.3638 mL | 1.8190 mL | 3.6380 mL | |
| 10 mM | 0.1819 mL | 0.9095 mL | 1.8190 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.
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