TīmeklisEZM 2302 (EZM2302, GSK 3359088) is a potent, selective, orally available arginine methyltransferase CARM1 inhibitor with IC50 of 6 nM, with broad selectivity against other HMTases; demonstrates in vitro anti-proliferative activity consistent with specific methyl mark inhibition with IC50 of <100 nM in 9/15 multiple myeloma cell lines, … Tīmeklis2024. gada 29. marts · EZM2302, GSK591, or SGC3027 treatment alone significantly inhibited the growth of MCF7, HCT116, and LNCaP cells, and their co-treatment …

EZM 2302 Cas# 1628830-21-6 - GlpBio

Tīmeklis2024. gada 22. maijs · EZM2302 also demonstrated antiproliferative activity of lymphoma cells in vitro and inhibited growth of multiple myeloma tumors in a mouse xenograft model . PRMT5 is overexpressed or upregulated in leukemia, lymphoma, and solid tumors, including glioblastoma and lung cancers [96, 112]. Tīmeklis2024. gada 21. dec. · EZM2302 is orally available with potent in vivo CARM1 inhibition. (a) Preclinical PK of EZM2302 in (a), CD-1 mouse and (b) Sprague-Dawley rat with or without jugular-and portal-vein cannulation ... mello which

Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo ...

TīmeklisEZM2302′s favorable physiochemical properties and ADME profile suggested its potential as an in vitro and in vivo tool compound. Finally, EPZ029751 was … TīmeklisEZM2302 showed dose-dependent exposure and tumor growth inhibition (TGI) after 21 days in the RPMI-8226 xenograft model. Tumors in all EZM2302 dose groups … Tīmeklis2024. gada 14. janv. · EZM 2302与CARM1结合，是CARM1活性的选择性抑制剂（IC50 = 6 nM），对其他组蛋白甲基转移酶具有广泛的选择性。. 用EZM 2302处理MM细胞系导致PABP1和SMB甲基化和细胞停滞的抑制，IC 50值在纳摩尔范围内（分别为9,31nM）。. EZM 2302抑制多种造血细胞系的体外增殖，第15天15个 ... naruto shippuden episode 192