Ombrabulin hydrochloride
Based on 1 Customer Validation
Ombrabulin hydrochloride is a derivative of CA-4 phosphate, which is known to exhibit antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.
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- Purity: 99.43%
- CAS No.: 253426-24-3
- 화학식: C21H27ClN2O6
- 분자량:438.90
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
tubulin[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
3.34 nM
Compound: AVE8062
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Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay
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[PMID: 26852340] |
| HeLa | IC50 |
0.0037 μM
Compound: 3, AC-7700
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Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
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[PMID: 19879758] |
| MCF7 | IC50 |
0.025 μM
Compound: 3, AC-7700
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Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
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[PMID: 19879758] |
| NCI-H460 | GI50 |
3.87 nM
Compound: AVE8062
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Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay
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[PMID: 26852340] |
| SK-OV-3 | GI50 |
3.96 nM
Compound: AVE8062
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Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay
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[PMID: 26852340] |
The effect of Ombrabulin (AVE8062) on endothelial or tumor cell viability is examined using the MTT assay. The IC50 of Ombrabulin for the mouse mesenteric endothelial cells (MMEC) is 10 nM and ranges between 7 and 20 nM for the tumor cell lines (HeyA8, SKOV3ip1, and HeyA8-MDR). Comparative analysis of the nonlinear least-squares regression of the dose-response curves for each agent alone and combination Ombrabulin /Docetaxel show a significantly lower IC50 than either agent alone (P<0.005, all cell lines). The cytotoxicity of Docetaxel is 2- to 4-fold greater in combination with Ombrabulin for the endothelial and tumor cells compared with Docetaxel alone[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 253426-24-3
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Appearance Solid
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분자량 438.90
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화학식 C21H27ClN2O6
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Color White to off-white
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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.[H]Cl
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Synonyms
AVE8062 hydrochloride; AC7700 hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 100 mg/mL (227.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 20 mg/mL (45.57 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
The capacity of Ombrabulin (AVE8062) to modulate MMEC and HeyA8 cell cycle as well as apoptosis is analyzed by flow cytometry. In all assays, 3×106 tumor cells are seeded into Petri dishes and allowed to adhere overnight. The cultures are then washed with PBS and treated with regular medium (negative control) or medium containing Docetaxel, Ombrabulin (HeyA8, 20 nM; MMEC 10 nM), or Ombrabulin plus Docetaxel. For cell cycle analyses, tumor cells are collected by trypsinization and pooled with the cells floating in the medium. The cell suspensions are centrifuged for 5 min at 1,500 rpm at room temperature, then washed and fixed with ethanol. For apoptosis analysis, cells are incubated overnight in 50 μL of DNA labeling solution (10 μL of reaction buffer, 0.75 μL of TdT enzyme, 8 μL of FITC-dUTP, and 32.25 μL of distilled water) at room temperature. Following the addition of rinse buffer, samples are centrifuged, washed, and fixed in ethanol. All samples are then washed with PBS, then resuspended in propidium iodide (50 μg/mL) and RNase A (20 μg/mL) in PBS for 30 min at room temperature. Stained cells are analyzed on an EPICS XL flow cytometer. The low-level gate is set at the base of the G1 peak and the percentages of cells within the G1 and G2-M phases of the cell cycle are determined by analysis with Multicycle[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female athymic nude mice (6-8 weeks old) are used. For in vivo injection, tumor cells are trypsinized, centrifuged at 1,000 rpm ×7 min at 4°C, washed twice, and resuspended in serum-free HBSS at a concentration of 5×106 cells/mL (SKOV3ip1 and HeyA8-MDR) and 1.25×106 cells/mL (HeyA8). Tumors are established by i.p. injection of cells. Ombrabulin therapy is initiated 7 or 17 days after cell line injection. Mice (n=10 per group) are randomly assigned to the following treatment groups: (a) PBS 200 μL, i.p. weekly; (b) Ombrabulin 30 mg/kg [dissolved in PBS (pH 5)] i.p. twice weekly; (c) Docetaxel 2 mg/kg (HeyA8 and HeyA8-MDR) or 1.4 mg/kg (SKOV3ip1) i.p. weekly; (d) Ombrabulin plus Docetaxel (both drugs given at the doses and frequency described above for each drug alone). The dose of Ombrabulin used in these experiments is optimized from dose-escalation studies against tumor growth. Mice are monitored for signs of adverse effects and tumors are harvested after treatment (range 2-5 weeks). The mouse weight, tumor weight, number of tumor nodules, and volume of ascites are recorded at necropsy.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (279 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.2784 mL | 11.3921 mL | 22.7842 mL | 56.9606 mL |
| 5 mM | 0.4557 mL | 2.2784 mL | 4.5568 mL | 11.3921 mL | |
| 10 mM | 0.2278 mL | 1.1392 mL | 2.2784 mL | 5.6961 mL | |
| 15 mM | 0.1519 mL | 0.7595 mL | 1.5189 mL | 3.7974 mL | |
| 20 mM | 0.1139 mL | 0.5696 mL | 1.1392 mL | 2.8480 mL | |
| 25 mM | 0.0911 mL | 0.4557 mL | 0.9114 mL | 2.2784 mL | |
| 30 mM | 0.0759 mL | 0.3797 mL | 0.7595 mL | 1.8987 mL | |
| 40 mM | 0.0570 mL | 0.2848 mL | 0.5696 mL | 1.4240 mL | |
| DMSO | 50 mM | 0.0456 mL | 0.2278 mL | 0.4557 mL | 1.1392 mL |
| 60 mM | 0.0380 mL | 0.1899 mL | 0.3797 mL | 0.9493 mL | |
| 80 mM | 0.0285 mL | 0.1424 mL | 0.2848 mL | 0.7120 mL | |
| 100 mM | 0.0228 mL | 0.1139 mL | 0.2278 mL | 0.5696 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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