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GSK3368715 dihydrochloride

🥰Excellent
Catalog No. T11500LCas No. 1628925-77-8
Alias GSK3368715 2HCl, EPZ019997 dihydrochloride, EPZ019997 2HCl

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.

GSK3368715 dihydrochloride

GSK3368715 dihydrochloride

🥰Excellent
Purity: 99.66%
Catalog No. T11500LAlias GSK3368715 2HCl, EPZ019997 dihydrochloride, EPZ019997 2HClCas No. 1628925-77-8
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.
Pack SizePriceAvailabilityQuantity
1 mg$56In Stock
1 mL x 10 mM (in DMSO)$94In Stock
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Purity:99.66%
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Product Introduction

Bioactivity
Description
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.
Targets&IC50
PRMT6:5.7 nM, PRMT3:48 nM, PRMT1:3.1 nM, PRMT4:1148 nM, PRMT8:1.7 nM
In vitro
In the majority of 249 cancer cell lines representing 12 tumor types, GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) exhibits 50% or more growth inhibition relative to DMSO-treated cells[1].
In vivo
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) markedly inhibits the growth of BxPC3 xenografts at all tested doses, achieving tumor growth reductions of 78% and 97% at 150 mg/kg and 300 mg/kg, respectively[1].
AliasGSK3368715 2HCl, EPZ019997 dihydrochloride, EPZ019997 2HCl
Chemical Properties
Molecular Weight439.46
FormulaC20H40Cl2N4O2
Cas No.1628925-77-8
SmilesCl.Cl.CCOCC1(COCC)CCC(CC1)c1n[nH]cc1CN(C)CCNC
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 100 mg/mL (227.55 mM), Sonication is recommended.
DMSO: 100 mg/mL (227.55 mM), Sonication is recommended.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.2755 mL11.3776 mL22.7552 mL113.7760 mL
5 mM0.4551 mL2.2755 mL4.5510 mL22.7552 mL
10 mM0.2276 mL1.1378 mL2.2755 mL11.3776 mL
20 mM0.1138 mL0.5689 mL1.1378 mL5.6888 mL
50 mM0.0455 mL0.2276 mL0.4551 mL2.2755 mL
100 mM0.0228 mL0.1138 mL0.2276 mL1.1378 mL

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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% 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 μLddH2OTargetMol | reagent mix well and clarify
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