EPZ-6438 (Tazemetostat)

Catalog No. A12712

EPZ-6438 (Tazemetostat)是一种有效的,选择性的,口服可利用的EZH2酶促活性小分子抑制剂,无细胞试验中Ki 和 IC50分别为2.5 nM 和 11 nM。它诱导SMARCB1缺失的MRT细胞中的凋亡和分化。
  • 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
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Catalog Num A12712
M. Wt 572.74
Formula C34H44N4O4
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 1403254-99-8
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
EPZ-6438 (Tazemetostat)是一种有效的,选择性的,口服可利用的EZH2酶促活性小分子抑制剂,无细胞试验中Ki 和 IC50分别为2.5 nM 和 11 nM。它诱导SMARCB1缺失的MRT细胞中的凋亡和分化。
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.