Ombrabulin
Based on 1 Customer Validation
Ombrabulin (AVE8062) is a derivative of CA-4 phosphate, which is known to exhibit antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.53%
- No. CAS: 181816-48-8
- Fòrmula: C21H26N2O6
- Peso molecular:402.44
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
tubulin[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Colon 26 | IC50 |
27.2 nM
Compound: 5a
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Antiproliferative activity against mouse Colon 26 cells assessed as inhibition of cell growth
Antiproliferative activity against mouse Colon 26 cells assessed as inhibition of cell growth
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[PMID: 23454513] |
| DU-145 | GI50 |
16.4 nM
Compound: 3' CA4-L-serinamide
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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 |
0.00072 μM
Compound: 20
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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] |
| HeLa | IC50 |
0.72 nM
Compound: 20
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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 |
0.0031 μM
Compound: 20
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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 |
24.1 nM
Compound: 3' CA4-L-serinamide
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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 |
9.02 nM
Compound: 3' CA4-L-serinamide
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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 (AC-7700) 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 (AC-7700)/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 (AC-7700) 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 181816-48-8
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Appearance Solid-Liquid Mixture
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Peso molecular 402.44
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Fòrmula C21H26N2O6
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Color White to light yellow
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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
AVE8062; AC7700
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (248.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (6.21 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (6.21 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
The capacity of Ombrabulin (AC-7700) 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 (AC-7700) (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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4848 mL | 12.4242 mL | 24.8484 mL | 62.1211 mL |
| 5 mM | 0.4970 mL | 2.4848 mL | 4.9697 mL | 12.4242 mL | |
| 10 mM | 0.2485 mL | 1.2424 mL | 2.4848 mL | 6.2121 mL | |
| 15 mM | 0.1657 mL | 0.8283 mL | 1.6566 mL | 4.1414 mL | |
| 20 mM | 0.1242 mL | 0.6212 mL | 1.2424 mL | 3.1061 mL | |
| 25 mM | 0.0994 mL | 0.4970 mL | 0.9939 mL | 2.4848 mL | |
| 30 mM | 0.0828 mL | 0.4141 mL | 0.8283 mL | 2.0707 mL | |
| 40 mM | 0.0621 mL | 0.3106 mL | 0.6212 mL | 1.5530 mL | |
| 50 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2424 mL | |
| 60 mM | 0.0414 mL | 0.2071 mL | 0.4141 mL | 1.0354 mL | |
| 80 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7765 mL | |
| 100 mM | 0.0248 mL | 0.1242 mL | 0.2485 mL | 0.6212 mL |
Ombrabulin Related Classifications
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