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EPZ-6438
60
CHF
CHF 60.00
In stock
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| Product Details | |
|---|---|
| Synonyms | Tazemetostat; E7438 |
| Product Type | Chemical |
| Properties | |
| 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 |
| InChi Key | NSQSAUGJQHDYNO-UHFFFAOYSA-N |
| 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. |
| Documents | |
| MSDS | Inquire |
| 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
- Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2: S.K. Knutson, et al.; PNAS 110, 7922 (2013)
- 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)
- 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)
- 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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