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RM-018
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RM-018图片
CAS NO:2641993-55-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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)

 

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.
分子量

985.22

性状

Solid

Formula

C56H72N8O8

CAS 号

2641993-55-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 60 mg/mL(60.90 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.0150 mL5.0750 mL10.1500 mL
5 mM0.2030 mL1.0150 mL2.0300 mL
10 mM0.1015 mL0.5075 mL1.0150 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。