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GSK4418959

🥰Excellent
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

GSK4418959

🥰Excellent
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 SizePriceAvailabilityQuantity
1 mg$413In Stock
5 mg$987In Stock
10 mg$1,590In Stock
25 mg$2,960In Stock
50 mg$4,550In Stock
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Product Introduction

Bioactivity
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].
SynonymsIDE275, IDE 275, GSK 4418959
Chemical Properties
Molecular Weight646.65
FormulaC31H30F4N4O5S
Cas No.3064599-36-3
Relative Density.no data available
ColorWhite
AppearanceSolid
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
DMSO: 80 mg/mL (123.71 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5464 mL7.7322 mL15.4643 mL77.3216 mL
5 mM0.3093 mL1.5464 mL3.0929 mL15.4643 mL
10 mM0.1546 mL0.7732 mL1.5464 mL7.7322 mL
20 mM0.0773 mL0.3866 mL0.7732 mL3.8661 mL
50 mM0.0309 mL0.1546 mL0.3093 mL1.5464 mL
100 mM0.0155 mL0.0773 mL0.1546 mL0.7732 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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