| Size | Price | Stock | Qty |
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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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| ln Vitro |
When it comes to the K562 human leukaemia cell line, isoalantolactone shows good cytotoxic action (IC50=1.2 μM) [1]. Using PANC-1, BxPC3, and HPAC cell lines, the cytotoxic effect of isoalantolactone on pancreatic cancer is assessed. A 24-hour dose-dependent inhibition of PANC-1 cell growth is seen upon isoalantolactone treatment. At 80 µM, the inhibition rate is greater than 90%, while 40 µM is the concentration required to provide 50% growth inhibition (IC50). When BxPC3 and HPAC cells are treated with isoalantolactone, a comparable pattern of cell viability reduction is shown, with IC50 values of 43 and 48 µM, respectively. Cell viability is restored by pretreatment with 3 mM N-Acetyl Cysteine (NAC), a particular ROS scavenger, suggesting that isoalantolactone has a harmful effect on cell viability by generating ROS[2].
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| ln Vivo |
The assessment of the acute and long-term harmful effects of isoalantolactone in CD1 mice is done by comparing the body weight, blood biochemistry, and liver and kidney histology of the animals to the control groups. Mice respond effectively to isoalantolactone, and at 100 mg/kg, there are no signs of pharmacotoxicity or mortality observed in either of the two trial periods (7 & 30 days). Throughout the two study periods, food consumption and body weight increases were similar in control and treated mice, and drug-related alterations in blood biochemistry and histopathological markers were not seen. Hematoxylin and eosin staining is used to evaluate the histological alterations in the liver and kidneys, and the results are associated with indicators of renal and liver function. There are no discernible morphological alterations in the kidney and liver structures of the treatment and control groups. On dosing day 7, the treatment group's serum levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) slightly increase, but this increase is not substantially different (P<0.05) from the control group. At dosing day 7, there is a statistically significant rise in the total bilirubin (TBIL) concentration in the treatment group (1.43±0.26 vs. 0.76±0.12 in the control, P<0.05). On dosing day 7, there is no significant difference (P<0.05) observed in the changes in renal function biomarkers between the control and treatment groups' serum. In the therapy group, there is a little increase in creatinine (Cr) concentration and a slight decrease in blood urea nitrogen (BUN) concentration. When mice receive a 30-day injection of isoalantolactone at a dose of 100 mg/kg, the serum levels of AST, ALT, TBIL, and BUN marginally decrease[2].
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| References | ||
| Additional Infomation |
Isoalantolactone is a sesquiterpene lactone of the eudesmanolide group. It has been isolated from Inula helenium. It has a role as an apoptosis inducer, an antifungal agent and a plant metabolite. It is a sesquiterpene lactone and a eudesmane sesquiterpenoid.
Isoalantolactone has been reported in Inula grandis, Carpesium macrocephalum, and other organisms with data available. |
| Molecular Formula |
C15H20O2
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|---|---|
| Molecular Weight |
242.32
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| Exact Mass |
232.146
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| CAS # |
470-17-7
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| PubChem CID |
73285
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
364.9±42.0 °C at 760 mmHg
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| Flash Point |
152.7±25.3 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.527
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
409
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@]12CCCC(=C)[C@@H]1C[C@H]3[C@@H](C2)OC(=O)C3=C
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| InChi Key |
CVUANYCQTOGILD-QVHKTLOISA-N
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| InChi Code |
InChI=1S/C15H20O2/c1-9-5-4-6-15(3)8-13-11(7-12(9)15)10(2)14(16)17-13/h11-13H,1-2,4-8H2,3H3/t11-,12+,13-,15-/m1/s1
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| Chemical Name |
(3aR,4aS,8aR,9aR)-8a-methyl-3,5-dimethylidene-3a,4,4a,6,7,8,9,9a-octahydrobenzo[f][1]benzofuran-2-one
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| Synonyms |
NSC-601353 NSC 601353 Isoalantolactone
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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 |
| 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 : ~100 mg/mL (~430.44 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.76 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 25.0 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: ≥ 2.5 mg/mL (10.76 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. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.76 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 | 4.1268 mL | 20.6339 mL | 41.2677 mL | |
| 5 mM | 0.8254 mL | 4.1268 mL | 8.2535 mL | |
| 10 mM | 0.4127 mL | 2.0634 mL | 4.1268 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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