EPZ011989 |
Catalog No.GC19141 |
EPZ011989 es un inhibidor potente y oralmente activo de Zeste Homolog 2 (EZH2) con estabilidad metabÓlica. EPZ011989 tiene una inhibiciÓn inhibitoria para EZH2 con un valor Ki de <3 nM. EPZ011989 muestra una fuerte inhibiciÓn de la marca de metilo y actividad antitumoral. EPZ011989 se puede utilizar para la investigaciÓn de varios tipos de cÁncer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1598383-40-4
Sample solution is provided at 25 µL, 10mM.
EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki 3000-fold selectivity over other HMTase.IC50 value: 15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
References:
[1]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.
Average Rating: 5
(Based on Reviews and 12 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *