| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| Targets |
Microtubule/Tubulin
|
|---|---|
| ln Vitro |
Combretastatin A-1 (72 h) suppresses the growth of a number of tumor cell lines in vitro, such as HepG2, SMMC-7721, Hepa 1-6, LM-3, Bel-7402, Huh7, BGC-803, MDA-MB-231, MCF-7, A375, NCI-1975, CT-26, HT-29, and A549 cells (IC50=9.2, 12.8, 32.9, 33.8, 38.4, 728.2, 12.2, 17.6, 46.0, 61.0, 256.3, 1075.0, 2082.0, 2247.0 nM, respectively)[2].
Combretastatin A-1 (1-10 nM; 24 h) causes apoptosis in HepG2 cells by eliminating GSK-3β inhibition and inducing AKT inactivation through microtubule depolymerization[2]. Combretastatin A-1 (1-50 nM; 6 h) reduces the HepG2 cells' mitochondrial membrane potential (MMP). ROS accumulation in HepG2 cells is dose-dependent when using Combretastatin A-1[2]. |
| ln Vivo |
Combretastatin A-1 (1-4 mg/kg; i.v. every other day for 4 weeks) dramatically reduces the tumor volume in HepG2 subcutaneous xenograft model[2].
Combretastatin A-1 (2 mg/kg; every other day for 21 days) exhibits increased apoptosis in orthotopic hepatocellular carcinoma mouse model[2]. |
| Cell Assay |
Cell Line: HepG2 cells
Concentration: 1, 5, 10 nM Incubation Time: 24 hours Result: Significantly decreased Mcl-1 expression, but the Bcl-2 level was unchanged. Reduced p-GSK 3β (Ser9) without altering total GSK-3β protein levels, indicating an activation of GSK-3β. Reduced AKT phosphorylation on Ser473 without an obvious change in the total AKT protein levels. |
| Animal Protocol |
Male athymic BALB/c nu/nu mice (16-18 g; 4-6 weeks old) were inoculated with HepG2 cells[2]
1, 2, 4 mg/kg I.v. every other day for 4 weeks |
| References |
|
| Molecular Formula |
C18H20O6
|
|---|---|
| Molecular Weight |
332.348
|
| Exact Mass |
332.12598835
|
| CAS # |
109971-63-3
|
| Related CAS # |
109971-63-3
|
| Appearance |
solid
|
| SMILES |
COC1=C(C(=C(C=C1)/C=C\C2=CC(=C(C(=C2)OC)OC)OC)O)O
|
| InChi Key |
YUSYSJSHVJULID-WAYWQWQTSA-N
|
| InChi Code |
InChI=1S/C18H20O6/c1-21-13-8-7-12(16(19)17(13)20)6-5-11-9-14(22-2)18(24-4)15(10-11)23-3/h5-10,19-20H,1-4H3/b6-5-
|
| Chemical Name |
3-methoxy-6-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]benzene-1,2-diol
|
| Synonyms |
Combretastatin A-1
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (~300.9 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.26 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 (6.26 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 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 (6.26 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 | 3.0089 mL | 15.0444 mL | 30.0888 mL | |
| 5 mM | 0.6018 mL | 3.0089 mL | 6.0178 mL | |
| 10 mM | 0.3009 mL | 1.5044 mL | 3.0089 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00960557 | Completed | Drug: Combretastatin A1 Diphosphate (OXi4503) |
Neoplasm Metastasis | Mateon Therapeutics | July 2009 | Phase 1 |
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