Dehydroaltenusin |
| Catalog No.GC35829 |
La déhydroalténusine est une petite molécule inhibitrice sélective de l'ADN polymérase eucaryote α, un type d'antibiotique produit par un champignon avec une valeur IC50 de 0,68 μM. Le mode d'action inhibiteur de la déhydroalténusine contre l'activité pol α des mammifères est compétitif par rapport À l'amorce matrice d'ADN (Ki = 0,23 μM) et non compétitif par rapport au substrat 2'-désoxyribonucléoside 5'-triphosphate (Ki = 0,18 μM) . La déhydroalténusine arrête le cycle cellulaire cancéreux en phase S et déclenche l'apoptose. La déhydroalténusine possède une activité antitumorale contre la tumeur de l'adénocarcinome humain in vivo.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 31186-13-7
Sample solution is provided at 25 µL, 10mM.
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Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM)[1].Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis[1].Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo[1]. IC50: 0.68 μM (DNA polymerase α)[1]
Dehydroaltenusin (38.0-44.4 μM; 24 hours) inhibits cell growth in a dose-dependent manner and the LD50 values varies from 38.0 to 44.4 μM[1].Dehydroaltenusin (38.0 μM; 6 hours) inhibits cell growth by blocking the S-phase of DNA replication[1].Dehydroaltenusin (75.0 μM; 24 hours) has a strong apoptotic effect on human cancer cells, DNA ladders can be detected after 12 h of incubation with dehydroaltenusin[1]. Cell Proliferation Assay[1] Cell Line: Human cancer cell line: A549, BALL-1, HeLa and NUGC-3 cells
Dehydroaltenusin (injection; 20 mg/kg; 2-day intervals; 12-39 days) shows suppressed tumor growth from 21 days[1]. Animal Model: Nude mice bearing HeLa solid tumors[1]
[1]. Mizushina Y, et al. Dehydroaltenusin is a specific inhibitor of mammalian DNA polymerase α. Expert Opin Investig Drugs. 2011 Nov;20(11):1523-34.
| Cas No. | 31186-13-7 | SDF | |
| Canonical SMILES | O=C(C(O)=C1)C=C(C2=CC(OC)=CC(O)=C23)[C@@]1(C)OC3=O | ||
| Formula | C15H12O6 | M.Wt | 288.25 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4692 mL | 17.3461 mL | 34.6921 mL |
| 5 mM | 0.6938 mL | 3.4692 mL | 6.9384 mL |
| 10 mM | 0.3469 mL | 1.7346 mL | 3.4692 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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