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EPZ020411 (hydrochloride)


CAS No. : 2070015-25-5

2070015-25-5
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Cat. No. : HY-12970A
M.Wt: 479.06
Formula: C25H39ClN4O3
Purity: >98 %
Solubility: DMSO : 50 mg/mL (ultrasonic);H2O : 20 mg/mL (ultrasonic;warming;heat to 60°C);0.1 M HCL : 50 mg/mL (ultrasonic;warming;adjust pH to 2 with HCl;heat to 60°C)
Introduction of 2070015-25-5 :

EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer[1][2]. IC50 & Target: IC50: 10 nM (PRMT6), 223 nM (PRMT8), 119 nM (PRMT1)[1] In Vitro: EPZ020411 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1].
EPZ020411 hydrochloride (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival[2]. In Vivo: EPZ020411 hydrochloride (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model[2].
1.19 Pharmacokinetic Parameters of EPZ020411 hydrochloride in rats[1].
Rats
IV 1 mg/kg		 Rats
SC 5 mg/kg
CL (mL/min/kg) 19.7±1.0
Vss (L/kg) 11.1±1.6
t1/2 (h) 8.54±1.43 9.19±1.60
tmax (h) 0.444
Cmax (ng/mL) 844±306
AUC0-τ (h·ng/mL) 745±34 2456±135
AUC0-inf (h·ng/mL) 846±45 2775±181
F (%) 65.6±4.3

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