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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $56 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $94 | - | In Stock |
| 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 | PRMT4:1148 nM, PRMT6:5.7 nM, PRMT1:3.1 nM, PRMT8:1.7 nM, PRMT3:48 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]. |
| Synonyms | GSK3368715 2HCl, EPZ019997 dihydrochloride, EPZ019997 2HCl |
| Molecular Weight | 439.46 |
| Formula | C20H40Cl2N4O2 |
| Cas No. | 1628925-77-8 |
| Smiles | Cl.Cl.CCOCC1(COCC)CCC(CC1)c1n[nH]cc1CN(C)CCNC |
| Relative Density. | no data available |
| Storage | store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 100 mg/mL (227.55 mM), Sonication is recommended. DMSO: 100 mg/mL (227.55 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.1 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
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