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Cephaeline

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Catalog No. TN1480Cas No. 483-17-0

Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis.

Cephaeline

Cephaeline

😃Good
Purity: 99.94%
Catalog No. TN1480Cas No. 483-17-0
Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$123In StockIn Stock
5 mg$263In StockIn Stock
10 mg$413In StockIn Stock
25 mg$673In StockIn Stock
50 mg$939In StockIn Stock
100 mg$1,260-In Stock
200 mg$1,680-In Stock
1 mL x 10 mM (in DMSO)$268In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.94%
Color:White to Yellow
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Product Introduction

Bioactivity
Description
Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis.
In vitro
We compared the transcriptomes of primary CLL cells cocultured or not with protective bone marrow stromal cells (BMSCs) and found that oxidative phosphorylation, mitochondrial function, and hypoxic signaling undergo most significant dysregulation in non-protected CLL cells, with the changes peaking at 6-8 h, directly before induction of apoptosis. A subset of CLL patients displayed a gene expression signature resembling that of cocultured CLL cells and had significantly worse progression-free and overall survival. To identify drugs blocking BMSC-mediated support, we compared the relevant transcriptomic changes to the Connectivity Map database. Correlation was found with the transcriptomic signatures of the cardiac glycoside ouabain and of the ipecac alkaloids emetine and Cephaeline. These compounds were highly active against protected primary CLL cells (relative IC50's 287, 190, and 35 nM, respectively) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis. We tested emetine in a murine model of CLL and observed decreased CLL cells in peripheral blood, spleen, and bone marrow, recovery of hematological parameters and doubling of median survival (31.5 vs. 15 days, P = 0.0001).
Chemical Properties
Molecular Weight466.61
FormulaC28H38N2O4
Cas No.483-17-0
Smiles[H][C@@]12C[C@H](C[C@H]3NCCc4cc(O)c(OC)cc34)[C@@H](CC)CN1CCc1cc(OC)c(OC)cc21
Relative Density.1.21g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 33.33 mg/mL (71.43 mM), Sonication is recommended.
DMSO: 100 mg/mL (214.31 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.57 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.1431 mL10.7156 mL21.4312 mL107.1559 mL
5 mM0.4286 mL2.1431 mL4.2862 mL21.4312 mL
10 mM0.2143 mL1.0716 mL2.1431 mL10.7156 mL
20 mM0.1072 mL0.5358 mL1.0716 mL5.3578 mL
50 mM0.0429 mL0.2143 mL0.4286 mL2.1431 mL
DMSO
1mg5mg10mg50mg
100 mM0.0214 mL0.1072 mL0.2143 mL1.0716 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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