1616391-65-1 EPZ015666 AKSci SYN3044
 
 
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  SYN3044    
EPZ015666
, >95%
 
EPZ-015666




IDENTITY
CAS Number:1616391-65-1
MF:C20H25N5O3
MW:383.44
SPECIFICATIONS & PROPERTIES
Purity:>95%
Physical Form:Powder
Long-Term Storage:Store long-term at 2-8°C

REVIEW

 Protein arginine methyltransferase-5 (PRMT5) is reported to have a role in diverse cellular processes, including tumorigenesis, and its overexpression is observed in cell lines and primary patient samples derived from lymphomas, particularly mantle cell lymphoma (MCL). EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity in biochemical assays with an IC50 of 22 nM and broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of December 13, 2019


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For research use only. Not for diagnostic or therapeutic use.
Not for human use.



PubChem