EZM 2302

1628830-21-6

C29H37ClN6O5

DMSO : >= 125 mg/mL (213.64 mM)

Epigenetics

EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC₅₀ of 6?nM. IC50 & Target: IC50: 6?nM (CARM1)^[1] In Vitro: EZM 2302 binds to CARM1 and is a selective inhibitor of CARM1 activity (IC₅₀=6?nM) with broad selectivity against other histone methyltransferases. Treatment of MM cell lines with EZM 2302 leads to inhibition of PABP1 and SMB methylation and cell stasis with IC₅₀ values in the nanomolar range (9, 31 nM, respectively). EZM 2302 inhibits the in vitro proliferation of multiple hematopoietic cell lines, with day 14 IC₅₀ values of less than 100?nM in 9 of 15 cell lines^[1]. In Vivo: EZM 2302 is stable in human hepatocytes (CL<3?mL/min/kg), and moderately binds to human, mouse and rat plasma proteins with a mean fraction unbound of 0.66, 0.46 and 0.74, respectively. In mouse and rat, the plasma clearance (CL) is 43 and 91?mL/min/kg, respectively. EZM 2302 shows dose-dependent exposure and tumor growth inhibition (TGI) after 21 days in the RPMI-8226 xenograft model. Tumors in all EZM 2302 dose groups measured on day 21 show significant decreases in tumor growth compared to vehicle^[1].