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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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GSK3368715 dihydrochloride (GSK-3368715; EPZ-019997; EPZ019997), the dihydrochloride salt of GSK3368715, is a potent and orally bioavailable inhibitor of type I PRMTs (protein arginine methyltransferases) with potential anticancer activity. It inhibits PRMT1/3/4/6/8 with IC50s of 3.1 nM, 48 nM, 1148 nM, 5.7 nM, 1.7 nM, respectively.
ln Vitro |
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) demonstrated 50% or greater growth inhibition in comparison to DMSO-treated cells in 249 cancer cell lines that represented 12 tumor types [1].
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ln Vivo |
At all tested doses, BxPC3 xenograft growth was significantly inhibited by GSK3368715 dihydrochloride (EPZ019997 dihydrochloride), which reduced tumor growth by 78% and 97% in the 150 mg/kg and 300 mg/kg dose groups, respectively. [1].
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References |
[1]. Fedoriw A, et al. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.
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Molecular Formula |
C₂₀H₄₀CL₂N₄O₂
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Molecular Weight |
439.46
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CAS # |
1628925-77-8
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Related CAS # |
GSK3368715;1629013-22-4;GSK3368715 trihydrochloride;2227587-26-8
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SMILES |
CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.[H]Cl.[H]Cl
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InChi Key |
HPSRPMOJFMXEKS-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H38N4O2.2ClH/c1-5-25-15-20(16-26-6-2)9-7-17(8-10-20)19-18(13-22-23-19)14-24(4)12-11-21-3/h13,17,21H,5-12,14-16H2,1-4H3,(H,22,23)2*1H
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Chemical Name |
N1-((3-(4,4-Bis(ethoxymethyl)cyclohexyl)-1H-pyrazol-4-yl)methyl)-N1,N2-dimethylethane-1,2-diamine dihydrochloride
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Synonyms |
EPZ019997 dihydrochlorideGSK 3368715 EPZ019997GSK3368715 EPZ-019997GSK-3368715 EPZ 019997
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~230 mg/mL (~523.37 mM)
H2O : ~140 mg/mL (~318.57 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (227.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2755 mL | 11.3776 mL | 22.7552 mL | |
5 mM | 0.4551 mL | 2.2755 mL | 4.5510 mL | |
10 mM | 0.2276 mL | 1.1378 mL | 2.2755 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.