product name EPZ015666
Description: EPZ015666, also known as GSK3235025, is is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models.
References: Nat Chem Biol. 2015 Jun;11(6):432-7.
383.44
Formula
C20H25N5O3
CAS No.
1616391-65-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 60 mg/mL (156.5 mM)
Water: <1 mg/mL
Ethanol: 48 mg/mL (125.2 mM)
Solubility (In vivo)
2% DMSO+30% PEG 300+ddH2O: 5 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models |
| Animal model | MCL (Z-138, and Maver-1) xenograft models |
| Formulation & Dosage | Dissolved in 0.5 % MC; 200 mg/kg; p.o. |
| References | Nat Chem Biol. 2015 Jun;11(6):432-7. |
