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5mg |
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10mg |
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Description: Ombrabulin (AVE8062; AC7700; AVE-8062) is an analogue of combretastatin A4 with improved water solubility, acting as a novel and potent tubulin inhibitor and vascular-disrupting agent with anticancer activity. It has better solubility and oral bioavailability, improved anti-cancer activity and decreased toxicity, and has been in 11 completed phase studies.
ln Vitro |
The MTT test is utilized to investigate the impact of Ombrabulin (AC-7700) on the viability of tumor or endothelial cells. For the tumor cell lines (HeyA8, SKOV3ip1, and HeyA8-MDR), ombrabulin's half-life (IC50) is 7–20 nM, while it is 10 nM for mouse mesenteric endothelial cells (MMEC). In comparison to each agent alone, Ombrabulin (AC-7700)/Docetaxel exhibits a considerably lower IC50 than either agent alone (P<0.005, all cell lines) according to a comparative analysis of the nonlinear least-squares regression of the dose-response curves. Compared to docetaxel alone, the cytotoxicity of cetaxel to tumor and endothelial cells is two to four times higher when combined with ombrabulin (AC-7700)[1].
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ln Vivo |
Prior to conducting therapeutic trials, the tolerance of two weekly intravenous, intraperitoneal, or subcutaneous injections of Ombabulin (AC-7700) at dosages ranging from 10 to 100 mg/kg is evaluated in nude mice (n = 3 per group). The IV and SC methods are not followed up on because of issues with tail vein necrosis or skin. With doses up to 100 mg/kg, the intraperitoneal route is well tolerated. Afterwards, pilot studies are conducted to ascertain the minimum dosage required for in vivo medicinal effectiveness. Tumor cell injection-bearing nude mice (n = 5 per group) are administered with vehicle or Ombrabulin 10, 30, 50, and 100 mg/kg twice weekly intraperitoneally (i.p.) for three weeks beginning seven days after the tumor cell injection. When comparing the 30 mg/kg group to the vehicle control group, there is a 65% decrease in tumor weight (P<0.02). The dosage of 10 mg/kg is ineffective. The 30 mg/kg dose is chosen for further therapy trials since the antitumor effects at doses higher than 30 mg/kg are not appreciably better[1].
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References |
[1]. Kim TJ, et al. Antitumor and antivascular effects of AVE8062 in ovarian carcinoma. Cancer Res. 2007 Oct 1;67(19):9337-45
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Molecular Formula |
C21H26N2O6
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Molecular Weight |
402.45
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Exact Mass |
402.1791
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CAS # |
181816-48-8
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Related CAS # |
Ombrabulin hydrochloride;253426-24-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(NC1=CC(/C=C\C2=CC(OC)=C(OC)C(OC)=C2)=CC=C1OC)[C@@H](N)CO
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Synonyms |
AVE 8062 AVE-8062 AVE8062
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4848 mL | 12.4239 mL | 24.8478 mL | |
5 mM | 0.4970 mL | 2.4848 mL | 4.9696 mL | |
10 mM | 0.2485 mL | 1.2424 mL | 2.4848 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.