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GSK864

🥰Excellent
Catalog No. T15442Cas No. 1816331-66-4
Alias GSK-864, GSK 864

GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases.

GSK864

GSK864

🥰Excellent
Purity: 97.07%
Catalog No. T15442Alias GSK-864, GSK 864Cas No. 1816331-66-4
GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases.
Pack SizePriceAvailabilityQuantity
1 mg$68In Stock
5 mg$163In Stock
10 mg$293In Stock
25 mg$579In Stock
50 mg$928In Stock
100 mg$1,480In Stock
1 mL x 10 mM (in DMSO)$197In Stock
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Purity:97.07%
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Product Introduction

Bioactivity
Description
GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases.
Targets&IC50
IDH1 (R132H):15.2 nM, 2-HG:320 nM (EC50), IDH1 (R132C):8.8 nM, IDH1 (R132G):16.6 nM
In vitro
GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells (EC50: 320 nM by LCMS/MS analysis) [1].
In vivo
In mice with R132C or R132H IDH1 mutant transplants treated with GSK864 (IP), the number of huCD45+ CD38+ cells showed a slight increase [1].
AliasGSK-864, GSK 864
Chemical Properties
Molecular Weight558.6
FormulaC30H31FN6O4
Cas No.1816331-66-4
SmilesCOc1c(C)cc(NC(=O)c2nn(Cc3ccc(F)cc3)c3c2CN(C[C@]3(C)C(N)=O)C(=O)c2ccc[nH]2)cc1C
Relative Density.1.37 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (179.02 mM), Sonication is recommended.
H2O: < 1 mg/mL (Insoluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7902 mL8.9509 mL17.9019 mL89.5095 mL
5 mM0.3580 mL1.7902 mL3.5804 mL17.9019 mL
10 mM0.1790 mL0.8951 mL1.7902 mL8.9509 mL
20 mM0.0895 mL0.4475 mL0.8951 mL4.4755 mL
50 mM0.0358 mL0.1790 mL0.3580 mL1.7902 mL
100 mM0.0179 mL0.0895 mL0.1790 mL0.8951 mL

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