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GSK3368715 dihydrochloride
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
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $56 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $94 | In Stock |
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Purity:99.66%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 | PRMT1:3.1 nM, PRMT6:5.7 nM, PRMT3:48 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]. |
| Alias | GSK3368715 2HCl, EPZ019997 dihydrochloride, EPZ019997 2HCl |
| Molecular Weight | 439.46 |
| Formula | C20H40Cl2N4O2 |
| Cas No. | 1628925-77-8 |
Storage & Solubility Information
| 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. | |||||||||||||||||||||||||||||||||||
| 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
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In Vivo Formulation Calculator (Clear solution)
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:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
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 (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.
(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 DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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