Valecobulin
Based on 1 Customer Validation
Valecobulin (CKD516) is a valine proagent of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.47%
- No. CAS: 1188371-47-2
- Fòrmula: C26H28N6O5S
- Peso molecular:536.60
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
β-tubulin polymerization[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
0.11 μM
Compound: 3
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Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
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[PMID: 20850313] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/C nu/nu mice (5-6 weeks of age) with HCT-116 or HCT-15 cells[1]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; administered on days 2, 6, 10, and 14
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Result:Had shown marked antitumor efficacy in various human tumor xenograft models.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1188371-47-2
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Appearance Solid
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Peso molecular 536.60
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Fòrmula C26H28N6O5S
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Color White to off-white
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SMILES
CC(C)[C@H](N)C(NC1=NC(C2=CC=C(C(C3=CC(OC)=C(OC)C(OC)=C3)=O)C(N4N=CN=C4)=C2)=CS1)=O
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Synonyms
CKD-516
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 125 mg/mL (232.95 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (3.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lee J, et al. Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors. J Med Chem. 2010 Sep 9;53(17):6337-54. [Content Brief]
[2]. Joo I, et al. Intravoxel incoherent motion diffusion-weighted MR imaging for monitoring the therapeutic efficacy of the vascular disrupting agent CKD-516 in rabbit VX2 liver tumors. Radiology. 2014 Aug;272(2):417-26. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8636 mL | 9.3179 mL | 18.6359 mL | 46.5896 mL |
| 5 mM | 0.3727 mL | 1.8636 mL | 3.7272 mL | 9.3179 mL | |
| 10 mM | 0.1864 mL | 0.9318 mL | 1.8636 mL | 4.6590 mL | |
| 15 mM | 0.1242 mL | 0.6212 mL | 1.2424 mL | 3.1060 mL | |
| 20 mM | 0.0932 mL | 0.4659 mL | 0.9318 mL | 2.3295 mL | |
| 25 mM | 0.0745 mL | 0.3727 mL | 0.7454 mL | 1.8636 mL | |
| 30 mM | 0.0621 mL | 0.3106 mL | 0.6212 mL | 1.5530 mL | |
| 40 mM | 0.0466 mL | 0.2329 mL | 0.4659 mL | 1.1647 mL | |
| 50 mM | 0.0373 mL | 0.1864 mL | 0.3727 mL | 0.9318 mL | |
| 60 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7765 mL | |
| 80 mM | 0.0233 mL | 0.1165 mL | 0.2329 mL | 0.5824 mL | |
| 100 mM | 0.0186 mL | 0.0932 mL | 0.1864 mL | 0.4659 mL |
Valecobulin Related Classifications
HY-13598 Related Classifications
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