Pemrametostat (GSK3326595, EPZ015938)是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5 (PRMT5)抑制剂,在体内外有效地抑制肿瘤生长。
MoreRalometostat (TNG908) is a potent, selective, and brain-penetrant PRMT5 inhibitor with an IC50 of 4 μM, exerting its effect through an MTA synergistic mechanism. It also demonstrates antitumor activity in xenograft models.
MoreMRTX1719 is a potent and selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5·MTA), which serves as a potential selective therapeutic target for tumor intervention.
MoreOnametostat (JNJ-64619178)是PRMT5抑制剂,具有较高的选择性和效力(PRMT5-MEP-50, IC50=0.14 nM)、良好的药代动力学特性以及安全性
MoreCopanlisib是一个高效的泛I型 PI3K抑制剂,其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3.
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