VU0155069
Based on 1 Customer Validation
VU0155069 (CAY10593), is a selective phospholipase D1 (PLD1) inhibitor with an IC50 value of 46 nM in vitro. VU0155069 (CAY10593) strongly inhibits the invasive migration of several cancer cell lines in transwell assays.
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- Pureza: 98.55%
- No. CAS: 1130067-06-9
- Fòrmula: C26H27ClN4O2
- Peso molecular:462.97
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Almacenamiento:Powder -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
- Pureza y Documentación
- Referencias
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Ver todos los productos específicos de isoformas Phospholipase
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Actividad biológica
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PLD1 46 nM (IC50) |
PLD2 933 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Calu-1 | IC50 |
11 nM
Compound: 69
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Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis
Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis
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[PMID: 19136975] |
| Calu-1 | IC50 |
46 nM
Compound: 3
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Inhibition of human PLD1 in Calu1 cells
Inhibition of human PLD1 in Calu1 cells
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[PMID: 19268584] |
| HEK293 | IC50 |
1800 nM
Compound: 69
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Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis
Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis
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[PMID: 19136975] |
| HEK293 | IC50 |
1800 nM
Compound: 13
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Inhibition of human GST-tagged PLD2A in human HEK293 cells
Inhibition of human GST-tagged PLD2A in human HEK293 cells
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[PMID: 20735042] |
| HEK293 | IC50 |
933 nM
Compound: 3
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Inhibition of GFP-labelled human PLD2 HEK293 cells
Inhibition of GFP-labelled human PLD2 HEK293 cells
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[PMID: 19268584] |
VU0155069 (0.5 μM, 1 h) significantly inhibits (R)-DOI (3 μM)-induced [3H]PtdBut production in MCF-7 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1130067-06-9
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Appearance Solid
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Peso molecular 462.97
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Fòrmula C26H27ClN4O2
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Color White to off-white
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SMILES
O=C(C1=CC=C2C=CC=CC2=C1)N[C@@H](C)CN3CCC(N4C5=CC=C(Cl)C=C5NC4=O)CC3
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Synonyms
CAY10593
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (108.00 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 (5.40 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.
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 (271 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]. Scott SA, et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol. 2009 Feb;5(2):108-17. [Content Brief]
[2]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1916-20. [Content Brief]
[3]. Barclay Z, et al. Attenuated PLD1 association and signalling at the H452Y polymorphic form of the 5-HT(2A) receptor. Cell Signal. 2013 Apr;25(4):814-21. [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, 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 | 2.1600 mL | 10.7998 mL | 21.5997 mL | 53.9992 mL |
| 5 mM | 0.4320 mL | 2.1600 mL | 4.3199 mL | 10.7998 mL | |
| 10 mM | 0.2160 mL | 1.0800 mL | 2.1600 mL | 5.3999 mL | |
| 15 mM | 0.1440 mL | 0.7200 mL | 1.4400 mL | 3.5999 mL | |
| 20 mM | 0.1080 mL | 0.5400 mL | 1.0800 mL | 2.7000 mL | |
| 25 mM | 0.0864 mL | 0.4320 mL | 0.8640 mL | 2.1600 mL | |
| 30 mM | 0.0720 mL | 0.3600 mL | 0.7200 mL | 1.8000 mL | |
| 40 mM | 0.0540 mL | 0.2700 mL | 0.5400 mL | 1.3500 mL | |
| 50 mM | 0.0432 mL | 0.2160 mL | 0.4320 mL | 1.0800 mL | |
| 60 mM | 0.0360 mL | 0.1800 mL | 0.3600 mL | 0.9000 mL | |
| 80 mM | 0.0270 mL | 0.1350 mL | 0.2700 mL | 0.6750 mL | |
| 100 mM | 0.0216 mL | 0.1080 mL | 0.2160 mL | 0.5400 mL |
VU0155069 Related Classifications
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