CHF 60.00
In stock
SYN-3045-M0011 mgCHF 60.00
SYN-3045-M0055 mgCHF 72.00
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Product Details
Synonyms Tazemetostat; E7438
Product Type Chemical
Formula C34H44N4O4
MW 572.8
CAS 1403254-99-8
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO.
Declaration Manufactured by SynKinase.
Other Product Data Target: EZH2 | Kinase Group: N/A | Substrate: N/A
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Specification Sheet
Datasheet Download PDF

EPZ6438 is a potent orally bioavailable, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 2.5nM), the enzymatic subunit of polycomb repressive complex It displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other histone methyltransferases. EPZ6438 blocks histone H3 lysine 27 trimethylation in both wild-type and mutant lymphoma cells (IC50 range from 2-90nM). EPZ6438 has been shown to induce apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor (MRT) cells and to promote their regression in xenograft-bearing mice.

Product References
  1. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2: S.K. Knutson, et al.; PNAS 110, 7922 (2013)
  2. Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma: S.K. Knutson, et al.; Mol. Cancer Ther. 13, 842 (2014)
  3. Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas: S.K. Knutson, et al.; PLoS One 9, e111840 (2014)
  4. EZH2 promotes colorectal cancer stem-like cell expansion by activating p21cip1-Wnt/β-catenin signaling: J.F. chen, et al.; Oncotarget (Epub ahead of print) (2016)
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