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Tazemetostat (EPZ-6438) hydrobromide is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
In vivo, Tazemetostat (250 or 500 mg/kg; twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors.
| Molecular Weight | 653.65 |
| Formula | C34H45BrN4O4 |
| CAS Number | 1467052-75-0 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone Methyltransferase Products |
|---|
| VTP50469
VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL Interaction with a Ki value of 104 pM. VTP50469 has anti-leukemia activity. |
| BIX 01294 Trihydrochloride
BIX 01294 Trihydrochloride is a potent inhitor of G9a histone methyltransferase with IC50 of 2.7 μM. |
| EBI-2511
EBI-2511 is an orally active, potent inhibitor of EZH2 in Pfeffiera cells IC50 The value is 6 nM. |
| EPZ-5676
EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase. |
| EPZ004777
EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50 of 0.4 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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