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$0.00 - Wang Z, .et al. Targeting EZH 2 as a novel therapeutic strategy for sorafenib‐resistant thyroid carcinoma, J Cell Mol Med, 2019, May 13 PMID: 31087496
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609 /
Biological Activity
EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
Targets
| EZH2 (Cell-free assay) | EZH2 (Cell-free assay) | |||
| 2.5 nM(Ki) | 2.5 nM(Ki) |
| In vitro (25°C) | DMSO | Warmed: 4 mg/mL (6.98 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 4% DMSO+30% PEG 300+5% Tween 80+ddH2O | 2.3 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 17.46 mL | 87.3 mL | 174.6 mL |
| 0.5 mM | 3.49 mL | 17.46 mL | 34.92 mL |
| 1 mM | 1.75 mL | 8.73 mL | 17.46 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.49 mL |
*The above data is based on the productmolecular weight 572.74. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A12712 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1403254-99-8 |
| Formula | C34H44N4O4 |
| M. Wt | 572.74 |
| Purity | >98% |
| Synonyms | EPZ6438, EPZ 6438 |
| SMILES | CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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