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EPZ015666

(CAS No:1616391-65-1)
EPZ015666(GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
CAS No:1616391-65-1
Molecular Weight(MW):383.44
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1616391-65-1
Molecular formula(MF) C20H25N5O3
Molecular Weight(MW): 383.44
Alias
Solubility
In vitro DMSO 60 mg/mL warmed (156.47 mM)
Ethanol 48 mg/mL warmed (125.18 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL
Biological Activity
Description EPZ015666(GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
Targets
PRMT5 [1]
5 nM(Ki)
In vitro

EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. [1]

In vivo EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. [1]