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GSK3368715

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Catalog No. T11500Cas No. 1629013-22-4
Alias EPZ019997

GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

GSK3368715

GSK3368715

😃Good
Catalog No. T11500Alias EPZ019997Cas No. 1629013-22-4
GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
Pack SizePriceAvailabilityQuantity
25 mg$2,72010-14 weeks
50 mg$3,58010-14 weeks
100 mg$4,90010-14 weeks
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Product Introduction

Bioactivity
Description
GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
Targets&IC50
PRMT8:1.7 nM , PRMT4:1148 nM , PRMT1:3.1 nM , PRMT6:5.7 nM , PRMT3:48 nM
In vitro
GSK3368715 ?shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types.
In vivo
GSK3368715 markedly impacts the growth of BxPC3 xenografts across all examined doses, achieving a reduction in tumor growth of 78% and 97% for the 150 mg/kg and 300 mg/kg dose groups, respectively.
AliasEPZ019997
Chemical Properties
Molecular Weight366.54
FormulaC20H38N4O2
Cas No.1629013-22-4
Relative Density.1.018 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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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 μLddH2OTargetMol | reagent mix well and clarify
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