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。
| 生物活性 | RM-018 is a potent, functionally distinct tricomplexKRASG12Cactive-state inhibitor. RM-018 retains the ability to bind and inhibit KRASG12C/Y96Dand could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRASG12C[1]. |
| IC50& Target[1] | KRAS (G12C) | KRAS (G12C/Y96D) |
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体外研究
(In Vitro) | 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].
Cell Viability Assay[1] | Cell Line: | NCI-H358, MIA PaCa-2, Ba/F3, and MGH1138-1 cells, which stably infected with KRASG12Cor KRASG12C/Y96D. | | Concentration: | 0.01-1000 nM | | Incubation Time: | 72 hours | | Result: | Inhibited the cell activity, but largely unaffected by KRASG12C/Y96Dexpression. |
Western Blot Analysis[1] | Cell Line: | MIA PaCa-2, HEK293T and MGH1138-1 cells, which expressing KRASG12Cor KRASG12C/Y96D. | | Concentration: | 0-100 nM | | Incubation Time: | 4 hours | | Result: | Inhibited KRAS, pERK and pRSK levels with similar potency. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 60 mg/mL(60.90 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.0150 mL | 5.0750 mL | 10.1500 mL | | 5 mM | 0.2030 mL | 1.0150 mL | 2.0300 mL | | 10 mM | 0.1015 mL | 0.5075 mL | 1.0150 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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