RM-018是一种KRAS抑制剂,它利用一种高度丰富的伴侣蛋白亲环蛋白a结合并抑制KRASG12C。 rm - 018(0.01 -1000海里;在NCI-H358、MIA PaCa-2、Ba/F3和MGH1138-1细胞中IC50s为1.4-3.5 nM (KRASG12C)和2.8-7.3 nM (KRASG12C/Y96D)。 rm - 018(0 - 100海里;4 h)抑制KRAS、pERK和pRSK蛋白的表达。
RM-018 is a “tricomplex” KRAS inhibitor, which exploits a highly abundant chaperone protein, cyclophilin A, to bind and inhibit KRAS G12C[1]. RM-018 (0.01-1000 nM; 72 hours) has IC 50 s of 1.4-3.5 nM (KRAS G12C ) and 2.8-7.3 nM (KRAS G12C/Y96D ) in NCI-H358, MIA ...
产品活性:RM-018 是一种 KRASG12C 活性状态的抑制剂。RM-018 保留了结合和抑制 KRASG12C/Y96D 的能力。RM-018 与 GTP-bound 结合,激活 KRASG12C 的[“RAS(ON)”] 状态。 研究领域:GPCR/G Protein 作用靶点:Ras In Vitro: RM-018 is a “tricomplex” KRAS inhibitor, which exploits a highly ab...