GSK3368715

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.

Catalog No. T11500Cas No. 1629013-22-4

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GSK3368715

Catalog No. T11500Cas No. 1629013-22-4

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Pack Size	Price	Availability
25 mg	$2,720	10-14 weeks
50 mg	$3,580	10-14 weeks
100 mg	$4,900	10-14 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.
Alias	EPZ019997

Chemical Properties

Molecular Weight	366.54
Formula	C₂₀H₃₈N₄O₂
Cas No.	1629013-22-4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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