RM-018
目录号: PL10857 纯度: ≥98%
CAS No. :2641993-55-5
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中文名称
RM-018
英文名称
RM-018
英文别名
RM-018
Cas No.
2641993-55-5
分子式
C56H72N8O8
分子量
985.22
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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 tricomplex KRAS active-state inhibitor. RM-018 retains the ability to bind and inhibit KRAS and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRAS.
性状
Solid
IC50 & Target[1][2]
KRAS (G12C) KRAS (G12C/Y96D)
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 KRAS.
RM-018 (0.01-1000 nM; 72 hours) has IC50s of 1.4-3.5 nM (KRAS) and 2.8-7.3 nM (KRAS) in NCI-H358, MIA PaCa-2, Ba/F3, and MGH1138-1 cells.
RM-018 (0-100 nM; 4 hours) inhibits the expression of KRAS, pERK, and pRSK protein. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献
[1]. Tanaka N, et.al. Clinical Acquired Resistance to KRAS 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.
溶解度数据
In Vitro: DMSO : 60 mg/mL (60.90 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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