1467052-75-0

1467052-75-0 structure

Name: Tazemetostat hydrobromide
Chemical Name: Tazemetostat hydrobromide
CAS Number: 1467052-75-0
Molecular Formula: C₃₄H₄₅BrN₄O₄
Molecular Weight: 653.65
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2019-12-29 17:44:38
Modify Date: 2024-01-09 17:57:10
Tazemetostat hydrobromide (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.

Name	Tazemetostat hydrobromide

Description	Tazemetostat hydrobromide (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.
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> Histone Methyltransferase
Target	EZH2 WT:2.5 nM (Ki) EZH2:11 nM (IC50, in peptide assay) EZH2:16 nM (IC50, in nucleosome assay) Rat EZH2:4 nM (IC50) EZH1:392 nM (IC50)
References	[1]. Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.

Molecular Formula	C₃₄H₄₅BrN₄O₄
Molecular Weight	653.65