RM-018
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。
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包装价格促销价数量
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5mg￥15487.0012390.00- +
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10mg￥25112.0020090.00- +
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25mg￥51300.0041040.00- +
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50mg￥80150.0064120.00- +
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100mg￥126112.00100890.00- +
- 货号: ajcx35924
- CAS: 2641993-55-5
- 别名:
- 分子式: C56H72N8O8
- 分子量: 985.22
- 纯度: ＞98%
- 溶解度:
- 储存: Store at -20°C
- 库存: 现货
Background
RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRASG12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active ["RAS(ON)"] state of KRASG12C[1].
RM-018 is a "tricomplex" KRAS inhibitor, which exploits a highly abundant chaperone protein, cyclophilin A, to bind and inhibit KRASG12C[1].RM-018 (0.01-1000 nM; 72 hours) has IC50s of 1.4-3.5 nM (KRASG12C) and 2.8-7.3 nM (KRASG12C/Y96D) in NCI-H358, MIA PaCa-2, Ba/F3, and MGH1138-1 cells[1].RM-018 (0-100 nM; 4 hours) inhibits the expression of KRAS, pERK, and pRSK protein[1].
[1]. Tanaka N, et.al. Clinical Acquired Resistance to KRASG12C Inhibition through a Novel KRAS Switch-II Pocket Mutation and Polyclonal Alterations Converging on RAS-MAPK Reactivation. Cancer Discov. 2021 Aug;11(8):1913-1922.
