A selective EZH2 inhibitor (IC50s = 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2

CPI-360 – 1 mg

Brand:
Cayman
CAS:
1802175-06-9
Storage:
-20
UN-No:
De Minimis - 3077 / 9

CPI-360 is a selective EZH2 inhibitor with IC50 values of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively.{29633} It decreases cellular levels of H3K27me3 and H3K27me2 (EC50s = 56 and 65 nM, respectively), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of non-Hodgkin’s lymphoma (NHL) cell lines.{29633} Twice daily, subcutaneous administration of 200 mg/kg of CPI-360 reduced tumor growth of KARPAS-422 xenografts in mice.{29633}  

 

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Description

A selective EZH2 inhibitor (IC50s = 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively); decreases cellular levels of H3K27me3 and H3K27me2 (EC50s = 56 and 65 nM, respectively), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of NHL cell lines

Formal name: N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-1H-indole-3-carboxamide

Synonyms: 

Molecular weight: 437.5

CAS: 1802175-06-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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