Tazemetostat hydrobromide

Modify Date: 2024-01-09 17:57:10

Tazemetostat hydrobromide Structure
Tazemetostat hydrobromide structure
Common Name Tazemetostat hydrobromide
CAS Number 1467052-75-0 Molecular Weight 653.65
Density N/A Boiling Point N/A
Molecular Formula C34H45BrN4O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Tazemetostat hydrobromide


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.

 Names

Name Tazemetostat hydrobromide

 Tazemetostat hydrobromide Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C34H45BrN4O4
Molecular Weight 653.65