EPZ015666(GSK3235025)
Catalog No.S7748 Synonyms: GSK3235025
Molecular Weight(MW): 383.44
EPZ015666(GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
Cited by 2 Publications
Purity & Quality Control
Choose Selective Histone Methyltransferase Inhibitors
Biological Activity
| Description | EPZ015666(GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. | ||
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| Targets |
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| In vitro |
EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. [1] |
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| In vivo | EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. [1] |
Protocol
| Cell Research: |
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| Animal Research: |
+ Expand
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Solubility (25°C)
| In vitro | DMSO | 60 mg/mL warmed (156.47 mM) |
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| Ethanol | 48 mg/mL warmed (125.18 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+ddH2O For best results, use promptly after mixing. |
5mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 383.44 |
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| Formula | C20H25N5O3 |
| CAS No. | 1616391-65-1 |
| Storage | powder |
| in solvent | |
| Synonyms | GSK3235025 |
Bio Calculators
Molarity Calculator
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
I want to use this compound for injection, how to reconstitute it?
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Answer:
S7748, EPZ015666 is a clear solution in 2% DMSO+30% PEG300+68% water and it can be used for tail vein injection.
