Opaganib
Based on 6 publication(s) in Google Scholar
Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
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- Pureza: 99.86%
- No. CAS: 915385-81-8
- Fòrmula: C23H25ClN2O
- Peso molecular:380.91
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Opaganib
More- Channels. 2020 Dec;14(1):216-230. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. [Abstract]
- FASEB J. 2019 Mar;33(3):3636-3646. [Abstract]
- Neurocrit Care. 2022 Apr;36(2):546-559. [Abstract]
- Arch Med Res. 2018 Jul;49(5):335-341. [Abstract]
- Oncotarget. 2016 Mar 29;7(13):16663-75. [Abstract]
Customer Validation & Images
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Actividad biológica
Ki: 9.8 μM (SK2)[1]
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Cell Line
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Type | Value | Description | References |
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| BXPC-3 | CC50 |
28.5 μM
Compound: 61; ABC294640
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Cytotoxicity against human BXPC-3 cells
Cytotoxicity against human BXPC-3 cells
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[PMID: 33539089] |
Using recombinant human SK1 and SK2, Opaganib demonstrates dose-dependent inhibition of SK2 with an IC50 of approximately 60 μM without affecting the activity of SK1 at concentrations up to at least 100 μM. In contrast, N,N-dimethylsphingosine (DMS) inhibits both SK1 and SK2 with IC50 values of approximately 60 and 20 μM, respectively. Kinetic analyses of varying concentrations of Opaganib (ABC294640) in the presence of 2.5 to 25 μM sphingosine indicated a Ki of 9.8±1.4 μM for the inhibition of SK2. Opaganib (ABC294640) decreases [3H]S1P formation in a dose-dependent fashion with an IC50 value of 26 μM[1]. IC50 values for Opaganib (ABC294640) are approximately 50 and 60 μM for A-498 and Bxpc-3 cells, respectively; whereas the IC50 values for Opaganib (ABC294640) are approximately 20 and 40 μM for these cells[2].
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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 915385-81-8
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Appearance Solid
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Peso molecular 380.91
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Fòrmula C23H25ClN2O
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Color White to off-white
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SMILES
O=C(C1(C2)CC3(C4=CC=C(Cl)C=C4)CC2CC(C3)C1)NCC5=CC=NC=C5
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Synonyms
ABC294640
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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
Publications (6)
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Journal Impact Factor
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Most Recent
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Channels
Sphingosine kinase 2 inhibitor ABC294640 suppresses neuronal excitability and inhibits multiple endogenously and exogenously expressed voltage-gated ion channels in cultured cells. [Abstract]2020 Dec;14(1):216-230. PMID: 32615066 -
Biochim Biophys Acta Mol Basis Dis
Sphingosine kinase 2 cooperating with Fyn promotes kidney fibroblast activation and fibrosis via STAT3 and AKT. [Abstract]2018 Nov;1864(11):3824-3836. PMID: 30251698
Opaganib purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. [Abstract]
NRK-49F cells are treated with TGF-β1 for the indicated time. The levels of p-STAT3, p-AKT, p-GSK3α, and p-GSK3β expression are detected in comparison with the levels of total STAT3, AKT, GSK3α, GSK3β, and with GAPDH as the loading control.
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FASEB J
Sphingosine kinase 2 promotes lipotoxicity in pancreatic β-cells and the progression of diabetes. [Abstract]2019 Mar;33(3):3636-3646. PMID: 30452878 -
Neurocrit Care
The Role of Sphingomyelin Metabolism in the Protection of Rat Brain Microvascular Endothelial Cells by Mild Hypothermia. [Abstract]2022 Apr;36(2):546-559. PMID: 34508278 -
Arch Med Res
Inhibition of SphK2 Stimulated Hepatic Gluconeogenesis Associated with Dephosphorylation and Deacetylation of STAT3. [Abstract]2018 Jul;49(5):335-341. PMID: 30448236
Opaganib purchased from MedChemExpress. Usage Cited in: Arch Med Res. 2018 Jul;49(5):335-341. [Abstract]
Inhibition of SphK2 by si-RNA (si-SphK2) and ABC294640 (ABC) decrease phosphorylation and acetylation of STAT3 . Also, both si-RNA and ABC294640 reverse IL-6 induced increasing phosphorylation and acetylation of STAT3.
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Oncotarget
Proteasomal degradation of sphingosine kinase 1 and inhibition of dihydroceramide desaturase by the sphingosine kinase inhibitors, SKi or ABC294640, induces growth arrest in androgen-independent LNCaP-AI prostate cancer cells. [Abstract]2016 Mar 29;7(13):16663-75. PMID: 26934645
Opaganib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Mar 29;7(13):16663-75. [Abstract]
The western blot demonstrates the effect of ABC294640 (25 μM) for 24 h in the presence and absence of MG132 (10 μM) on Des1 expression. Actin is used a protein loading control.
Solvente y solubilidad
DMSO : 100 mg/mL (262.53 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 (6.56 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 (6.56 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.
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
To determine the effects of the test compounds (e.g., Opaganib (ABC294640)) on proliferation, cells are plated into 96-well microtiter plates and allowed to attach for 24 h. Varying concentrations of Opaganib are added to individual wells and the cells are incubated for an additional 72 h. At the end of this period, the number of viable cells is determined by use of the sulforhodamine-binding assay. The percentage of cells killed is calculated as the percentage decrease in sulforhodamine-binding compare with control cultures. Regression analyses of inhibition curves are performed by use of GraphPad Prism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Sprague-Dawley male rats (7-8 weeks old) are orally dosed with 0, 100, or 250 mg of ABC294640•HCl/kg in 0.375% Polysorbate-80 in PBS daily for 7 days. The animals are observed daily for viability, signs of gross toxicity, and behavioral changes, and a battery of detailed observations are performed on study days 1 and 7. Blood is sampled from all animals on day 8 of the study for hematology, clinical biochemistry, and serology assessments, and the animals are sacrificed. Gross necropsies are performed on all study rats, and selected organs and tissues are evaluated in the control and high-dose level groups.
Mice[3]
Male C57BL/6 (8-9 weeks) mice are gavaged with 50 mg/kg of Opaganib (ABC294640), or an equivalent volume of vehicle (0.375% Tween 80 in phosphate buffered saline, pH 7.1) 1 h before surgery. Under ether anesthesia, ischemia to 70% of the total liver is induced for 1 h. After opening the vascular clamp, the non-ischemic liver lobes are removed, and mice are observed 7 days for survival. Sham operation included equivalent anesthesia and laparotomy without ischemia.
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 (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. French KJ, et al. Pharmacology and antitumor activity of ABC294640, a selective inhibitor of sphingosine kinase-2. J Pharmacol Exp Ther. 2010 Apr;333(1):129-39. [Content Brief]
[2]. Beljanski V, et al. Combined anticancer effects of sphingosine kinase inhibitors and sorafenib. Invest New Drugs. 2011 Dec;29(6):1132-42. [Content Brief]
[3]. Shi Y, et al. Sphingosine kinase-2 inhibition improves mitochondrial function and survival after hepatic ischemia-reperfusion. J Hepatol. 2012 Jan;56(1):137-45. [Content Brief]
[4]. Liu Q, et al. Inhibition of sphingosine kinase-2 suppresses inflammation and attenuates graft injury after liver transplantation in rats. PLoS One. 2012;7(7):e41834. [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 |
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| DMSO | 1 mM | 2.6253 mL | 13.1265 mL | 26.2529 mL | 65.6323 mL |
| 5 mM | 0.5251 mL | 2.6253 mL | 5.2506 mL | 13.1265 mL | |
| 10 mM | 0.2625 mL | 1.3126 mL | 2.6253 mL | 6.5632 mL | |
| 15 mM | 0.1750 mL | 0.8751 mL | 1.7502 mL | 4.3755 mL | |
| 20 mM | 0.1313 mL | 0.6563 mL | 1.3126 mL | 3.2816 mL | |
| 25 mM | 0.1050 mL | 0.5251 mL | 1.0501 mL | 2.6253 mL | |
| 30 mM | 0.0875 mL | 0.4375 mL | 0.8751 mL | 2.1877 mL | |
| 40 mM | 0.0656 mL | 0.3282 mL | 0.6563 mL | 1.6408 mL | |
| 50 mM | 0.0525 mL | 0.2625 mL | 0.5251 mL | 1.3126 mL | |
| 60 mM | 0.0438 mL | 0.2188 mL | 0.4375 mL | 1.0939 mL | |
| 80 mM | 0.0328 mL | 0.1641 mL | 0.3282 mL | 0.8204 mL | |
| 100 mM | 0.0263 mL | 0.1313 mL | 0.2625 mL | 0.6563 mL |
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