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%
This product is discontinued due to commercial reason. Tazemetostat (formerly known as EPZ-6438 or E7438; Tazverik) is an orally bioavailable, potent, and selective EZH2 (Enhancer of Zeste-Homolog 2) inhibitor with antineoplastic activity. It inhibits EZH2 with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays. As of Jan 23, 2020, Tazemetostat was approved for the treatment of metastatic or locally advanced epithelioid sarcoma not eligible for complete resection. Mutations within the catalytic domain of the histone methyltransferase EZH2 have been identified in subsets of patients with non-Hodgkin lymphoma (NHL). These genetic alterations are hypothesized to confer an oncogenic dependency on EZH2 enzymatic activity in these cancers. Tazemetostat exhibits a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.Tazemetostat competitively binds to the S-adenosylmethionine (SAM) binding site of EZH2 and also non-competitively binds to the binding sites of peptide or nucleosome substrate. Tazemetostat selectively inhibits EZH2 with selectivity 35-fold greater than EZH1. Study results have suggested that Tazemetostat exhibits dramatic and permanent anti-tumor activity in MRT models through synergistic effects of Tazemetostat-mediated EZH2 inhibition on several cancer pathways.
ln Vitro |
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ln Vivo |
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Animal Protocol |
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References |
Proc Natl Acad Sci U S A.2013 May 7;110(19):7922-7
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Molecular Formula |
C34H44N4O4
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Molecular Weight |
572.74
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CAS # |
1403254-99-8
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Related CAS # |
1467052-84-1 (HCl);1467052-75-0 (HBr);1403254-99-8;
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SMILES |
O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O
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Chemical Name |
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
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Synonyms |
Tazemetostat; E7-438; EPZ 6438; E 7438; EPZ6438; tazerik; E7438; EPZ-6438;
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7460 mL | 8.7300 mL | 17.4599 mL | |
5 mM | 0.3492 mL | 1.7460 mL | 3.4920 mL | |
10 mM | 0.1746 mL | 0.8730 mL | 1.7460 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05228158 | Recruiting | Drug: Tazemetostat | Lymphoma, Follicular | Eisai Co., Ltd. | August 16, 2021 | |
NCT05934838 | Recruiting | Drug: Tazemetostat Pill | Follicular Lymphoma B-Cell Lymphoma |
Weill Medical College of Cornell University |
October 4, 2023 | Phase 1 |
NCT05023655 | Recruiting | Drug: Tazemetostat | Solid Tumor ARID1A Gene Mutation |
Prisma Health-Upstate | January 6, 2022 | Phase 2 |
NCT05994235 | Recruiting | Drug: Mosunetuzumab Drug: Tazemetostat Pill |
Follicular Lymphoma | Weill Medical College of Cornell University |
November 1, 2023 | Phase 2 |
EPZ-6438 eradicates SMARCB1-deleted MRT xenografts in SCID mice.Proc Natl Acad Sci U S A. 2013 May 7; 110(19): 7922–7927. |
Effects of EPZ-6438 on cellular global histone methylation and cell viability.Proc Natl Acad Sci U S A. 2013 May 7; 110(19): 7922–7927. td> |
EPZ-6438 induces changes in expression of SMARCB1-regulated genes and cell morphology.Proc Natl Acad Sci U S A. 2013 May 7; 110(19): 7922–7927. td> |