Size | Price | Stock | Qty |
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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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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
EPZ015866 (also known as EPZ-015866; GSK-3203591; GSK-591) is an orally bioavailable and selective inhibitor of PRMT5 (protein arginine methyltransferase 5) with potential anticancer activity. EPZ015866 was discovered based on the precursor and analog EPZ015666 (GSK3235025).
ln Vitro |
Treatment with GSK591 (5 μM; MCF7, T47D, and MCF10A cells) inhibits the proliferation and self-renewal of breast cancer stem cells (BCSCs). In vitro, GSK591 lowers the quantity of BCSCs[2].
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ln Vivo |
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Cell Assay |
Cell Proliferation Assay[2]
Cell Types: MCF7, T47D, and MCF10A cells Tested Concentrations: 5 μM Incubation Duration: Experimental Results: Suppressed BCSCs proliferation and self-renewal. |
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Animal Protocol |
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References |
[1]. Kenneth W. Duncan et al. Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. ACS Med. Chem. Lett., 2016, 7 (2), pp 162-166.
[2]. Chiang K, et al. PRMT5 Is a Critical Regulator of Breast Cancer Stem Cell Function via Histone Methylation and FOXP1 Expression. Cell Rep. 2017 Dec 19;21(12):3498-3513. |
Molecular Formula |
C22H28N4O2
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Molecular Weight |
380.48
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CAS # |
1616391-87-7
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Related CAS # |
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SMILES |
O=C(NC[ C@H](O)CN1CCC(C=CC=C2)=C2C1)C3=CC(NC4CCC4)=NC=C3
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.91 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 22.5 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: ≥ 2.25 mg/mL (5.91 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 22.5 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: ≥ 2.25 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL | |
5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL | |
10 mM | 0.2628 mL | 1.3141 mL | 2.6283 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.
Co-crystal structures of PRMT5:MEP50 (green) with compound8(A, magenta), compound9(B, orange), compound10(C, yellow), and compound15(D, cyan).ACS Med Chem Lett.2015 Dec 2;7(2):162-6. th> |
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Plot of cLogD vs scaled clearance (CL) from human microsomes (A) and mouse liver microsomes (B).Plot of proliferation IC50in Z-138 cells vs observed CL in mouse PK (C) and percentage oral bioavailability %F from mouse PK (D) dosed at 2 mg/kg IV and 10 mg/kg PO.ACS Med Chem Lett.2015 Dec 2;7(2):162-6. td> |
Plasma PK profile ofEPZ015666in male CD-1 mouse following single dose administration at 10 and 100 mg/kg p.o. Methyl mark IC90corrected for PPB shown as dotted line. ACS Med Chem Lett.2015 Dec 2;7(2):162-6. td> |