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Linderalactone is a naturally occurring sesquiterpene lactone isolated from Radix linderae with anticancer activity by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway.
ln Vitro |
A549 cells treated with suspension doses for 24 hours showed growth inhibition from endomelide (0-100 μM). Hegenolide's IC50 is 15 μM[1]. Treatment of A549 cells with linderalactone (7.5-30 μM) causes cell fluorescence. A549 cells are treated with linderalactone (7.5-30 μM; 24 hours) to trigger the G2/M cell cycle. A549 cells are anesthetized by linderalactone (7.5–30 μM), which works in a dose-dependent manner[1]. suppresses the expression of JAK1, JAK2, and STAT1. Additionally, phosphorylation of pSTAT1, pSTAT-2, pJAK1, and pJAk2 can be inhibited by hierastrolide [1].
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Cell Assay |
Cell viability assay [1]
Cell Types: lung cancer A549 cells Tested Concentrations: 0 μM, 1]. 1.6 μM, 3.2 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Concentration-dependent inhibition of A549 cell growth. Apoptosis analysis [1] Cell Types: lung cancer A549 cells Tested Concentrations: 7.5 μM, 15 μM, 30 μM Incubation Duration: Experimental Results: Induced apoptosis of A549 cells in a dose-dependent manner. Cell cycle analysis [1] Cell Types: Lung cancer A549 cells Tested Concentrations: 7.5 μM, 15 μM, 30 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced G2/M cell cycle arrest. Western Blot Analysis [1] Cell Types: lung cancer A549 cells Tested Concentrations: 7.5 μM, 15 μM, 30 μM Incubation Duration: Experimental Results: Inhibition of JAK/STAT pathway in A549 cells. |
References |
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Additional Infomation |
Linderalactone has been reported in Neolitsea zeylanica, Neolitsea hiiranensis, and other organisms with data available.
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Molecular Formula |
C15H16O3
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Molecular Weight |
244.2857
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Exact Mass |
244.109
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CAS # |
728-61-0
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PubChem CID |
6450191
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Appearance |
White to yellow solid powder
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Density |
1.2±0.1 g/cm3
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Boiling Point |
437.9±45.0 °C at 760 mmHg
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Flash Point |
218.6±28.7 °C
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Vapour Pressure |
0.0±1.1 mmHg at 25°C
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Index of Refraction |
1.572
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LogP |
3.27
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
3
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Rotatable Bond Count |
0
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Heavy Atom Count |
18
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Complexity |
422
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Defined Atom Stereocenter Count |
1
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SMILES |
C/C/1=C\CCC2=C[C@H](C3=C(C1)OC=C3C)OC2=O
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InChi Key |
LWCKQMHMTSRRAA-QGQQYVBWSA-N
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InChi Code |
InChI=1S/C15H16O3/c1-9-4-3-5-11-7-13(18-15(11)16)14-10(2)8-17-12(14)6-9/h4,7-8,13H,3,5-6H2,1-2H3/b9-4+/t13-/m1/s1
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Chemical Name |
(1R,8E)-3,8-dimethyl-5,14-dioxatricyclo[10.2.1.02,6]pentadeca-2(6),3,8,12(15)-tetraen-13-one
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
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 : ~33.33 mg/mL (~136.44 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (10.23 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 sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.23 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.0935 mL | 20.4675 mL | 40.9350 mL | |
5 mM | 0.8187 mL | 4.0935 mL | 8.1870 mL | |
10 mM | 0.4093 mL | 2.0467 mL | 4.0935 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.