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EPZ-6438

  • EPZ-6438 200x200
  • EPZ-6438 600x600
Price:
$129.00
Catalog #:
C3764-5
Quantity:


Product Description

EPZ-6438 is a potent, selective and orally bioavailable inhibitor of methyltransferase EZH2 with a Ki value of 2.5 nM. EPZ-6438 also shows a 35-fold selectivity versus EZH1 (IC50 392 nM) and >4,500-fold selectivity relative to 14 other histone methyltransferases (HMTs). [1] Oral dosing of EPZ-6438 leads to potent antitumor activity in a SMARCB1-deleted malignant rhabdoid tumor (MRT) xenograft model. [1]
EPZ-6438 is being studied in Phase III clinical trials in patients with diffuse large B-cell lymphoma [2] and relapsed/refractory synovial sarcoma [3].


Technical information:

Chemical Formula:   C34H44N4O4
CAS #:   1403254-99-8
Molecular Weight:   572.74
Purity:   > 98%
Appearance:   Off-white
Chemical Name:   N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide
Solubility:   Up to 10 nM in DMSO
Synonyms:   EPZ-6438, EPZ6438, Tazemetostat

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.


Reference:

1. Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci U S A. 2013; 110(19):7922-7 Pubmed ID: 23620515
2. Open-Label, Multicenter, Phase 1/2 Study of Tazemetostat (EZH2 Histone Methyl Transferase [HMT] Inhibitor) as a Single Agent in Subjects With Adv. Solid Tumors or With B-cell Lymphomas and Tazemetostat in Combination With Prednisolone in Subjects With DLBCL.  clinicaltrials.gov/NCT01897571 
3.

A Phase II, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adult Subjects With INI1-Negative Tumors or Relapsed/Refractory Synovial Sarcoma. clinicaltrials.gov/NCT02601950


Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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