EPZ005687

Alias: EPZ 005687; EPZ-005687; EPZ005687; EPZ-5687; EPZ 5687; EPZ5687.
Cat No.:V0379 Purity: ≥98%
EPZ005687 (EPZ-005687) is a novel, potent and selective inhibitor of EZH2 (a histone lysine N-methyltransferase) with anticancer activity.
EPZ005687 Chemical Structure CAS No.: 1396772-26-1
Product category: Histone Methyltransferase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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].
ln Vivo
Intra-articular injection of EPZ005687 delayed OA development in mice.
Animal Protocol
5.6 μM, 50 μL; intra-articular injection
Osteoarthritis (OA) mouse model
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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C32H37N5O3
Molecular Weight
539.67
CAS #
1396772-26-1
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]
InChi Key
ZOIBZSZLMJDVDQ-UHFFFAOYSA-N
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)
Chemical Name
1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide.
Synonyms
EPZ 005687; EPZ-005687; EPZ005687; EPZ-5687; EPZ 5687; EPZ5687.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 2 mg/mL (3.7 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.

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