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GSK4418959
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Catalog No. T204089Cas No. 3064599-36-3
Alias IDE275, IDE 275, GSK 4418959
GSK4418959 (IDE275) is a non-covalent, reversible, selective, and orally active inhibitor of the Werner syndrome helicase (WRN helicase). GSK4418959 inhibits both ATPase and DNA unwinding activities of WRN helicase in an ATP-competitive manner. GSK4418959 is a valuable chemical tool for the study of microsatellite instability-high (MSI-H) cancers, where WRN helicase plays an essential role in maintaining genomic stability.
GSK4418959
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Purity: 99.14%
Catalog No. T204089Alias IDE275, IDE 275, GSK 4418959Cas No. 3064599-36-3
GSK4418959 (IDE275) is a non-covalent, reversible, selective, and orally active inhibitor of the Werner syndrome helicase (WRN helicase). GSK4418959 inhibits both ATPase and DNA unwinding activities of WRN helicase in an ATP-competitive manner. GSK4418959 is a valuable chemical tool for the study of microsatellite instability-high (MSI-H) cancers, where WRN helicase plays an essential role in maintaining genomic stability.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $372 | In Stock | In Stock | |
| 5 mg | $892 | In Stock | In Stock | |
| 10 mg | $1,320 | In Stock | In Stock | |
| 25 mg | $2,480 | - | In Stock | |
| 50 mg | $3,790 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $1,290 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.14%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | GSK4418959 (IDE275) is a non-covalent, reversible, selective, and orally active inhibitor of the Werner syndrome helicase (WRN helicase). GSK4418959 inhibits both ATPase and DNA unwinding activities of WRN helicase in an ATP-competitive manner. GSK4418959 is a valuable chemical tool for the study of microsatellite instability-high (MSI-H) cancers, where WRN helicase plays an essential role in maintaining genomic stability. |
| In vivo | GSK4418959 (IDE275) induces tumor regression and activates DNA damage response (DDR) markers in several MSI-H CDX and PDX models across diverse tumor types, including CRC, endometrial, and gastric cancers with varying oncogenic drivers and tumor suppressor mutations, while sparing MSS models[1]. |
| Synonyms | IDE275, IDE 275, GSK 4418959 |
| Molecular Weight | 646.65 |
| Formula | C31H30F4N4O5S |
| Cas No. | 3064599-36-3 |
| Smiles | C(O)(=O)[C@@H]1[C@H](CCC[C@H]1C(NC2=C(F)C=C(C(F)(F)F)C=C2)=O)C3=CC=C(N(S(=O)(=O)C=4C=C5C(=CC4)N(C)C(C)=N5)C)C=C3 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (123.71 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
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:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
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 DMSO 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 DMSO stock solution to 400 μL PEG300 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 ddH2O 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.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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