| References: |
EPZ015666 is the first-in-class PRMT5 inhibitor showing in vitro and in vivo 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.EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. EPZ015666 demonstrated potent killing of cancer cells in vitro and efficacy in animal models of MCL, with correlation to methyl mark inhibition. EPZ01566 is orally bioavailable and demonstrated dose-dependent inhibition of intracellular symmetric arginine di-methylation of SmD3, a PRMT5 substrate that plays a critical role in RNA processing. In pre-clinical studies, Z138 and Maver MCL cell lines were shown to be sensitive to EPZ015666, and in xenografts of these cell lines, the compound showed dose-dependent tumor growth inhibition.
For the detailed information of EPZ015666, the solubility of EPZ015666 in water, the solubility of EPZ015666 in DMSO, the solubility of EPZ015666 in PBS buffer, the animal experiment (test) of EPZ015666, the cell expriment (test) of EPZ015666, the in vivo, in vitro and clinical trial test of EPZ015666, the EC50, IC50,and affinity,of EPZ015666, Please contact DC Chemicals. |
