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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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Purity: ≥98%
EPZ005687 (EPZ-005687) is a novel, potent and selective inhibitor of EZH2 (a histone lysine N-methyltransferase) with anticancer activity. It inhibits EZH2 with a Ki of 24 nM in a cell-free assay, and displays >50-fold higher selectivity for EZH2 over EZH1 and 15 other protein methyltransferases. EPZ005687 demostrates potent in vitro antiproliferative activity and high in vivo antitumor efficacy.
ln Vitro |
EPZ005687 exhibits an IC50 value of 54±5 nM, indicating concentration-dependent reduction of PRC2 enzymatic activity. H3K27 methylation in lymphoma cells is particularly inhibited by EPZ005687. The proliferation of the EZH2Y641F-bearing cell line is significantly impacted by EPZ005687. In mutant EZH2 lymphoma cells, but not in wild-type cells, EPZ005687 inhibits proliferation[1]. U937 cells undergo a clear apoptosis in response to EPZ005687 at doses of 0.5, 1, 5, and 10 µM. The proliferation of U937 cells is clearly inhibited by EPZ005687, whereas NBMCD34+ cell growth is very slightly affected. EPZ005687 causes blockage of the G1 phase and reduces the proportion of S phase cells in U937 cells. Furthermore, H3K27 methylation in U937 cells is clearly depleted by EPZ005687, whereas H3K27 methylation in NBMCD34+ cells is barely affected[2].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Knutson SK, et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012;8(11):890-6.
[2]. Tang SH, et al. Effects of H3K27 methylation inhibitor EPZ005687 on apoptosis, proliferation and cell cycle of U937 cells and normal CD34 positive cells. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Dec;22(6):1561-6 |
Molecular Formula |
C32H37N5O3
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Molecular Weight |
539.67
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CAS # |
1396772-26-1
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SMILES |
O1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])C1=C([H])C(C(N([H])C([H])([H])C2C(N([H])C(C([H])([H])[H])=C([H])C=2C([H])([H])[H])=O)=O)=C2C([H])=NN(C2=C1[H])C1([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
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InChi Key |
ZOIBZSZLMJDVDQ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C32H37N5O3/c1-21-15-22(2)35-32(39)28(21)18-33-31(38)27-16-25(17-30-29(27)19-34-37(30)26-5-3-4-6-26)24-9-7-23(8-10-24)20-36-11-13-40-14-12-36/h7-10,15-17,19,26H,3-6,11-14,18,20H2,1-2H3,(H,33,38)(H,35,39)
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Chemical Name |
1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide.
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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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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8530 mL | 9.2649 mL | 18.5298 mL | |
5 mM | 0.3706 mL | 1.8530 mL | 3.7060 mL | |
10 mM | 0.1853 mL | 0.9265 mL | 1.8530 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.