1. GPCR/G Protein
  2. Ras
  3. RM-018

RM-018 

Cat. No.: HY-141477
Handling Instructions

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.

For research use only. We do not sell to patients.

RM-018 Chemical Structure

RM-018 Chemical Structure

CAS No. : 2641993-55-5

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Description

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].

IC50 & Target[1]

KRAS (G12C)

 

KRAS (G12C/Y96D)

 

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: NCI-H358, MIA PaCa-2, Ba/F3, and MGH1138-1 cells, which stably infected with KRASG12C or KRASG12C/Y96D.
Concentration: 0.01-1000 nM
Incubation Time: 72 hours
Result: Inhibited the cell activity, but largely unaffected by KRASG12C/Y96D expression.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2, HEK293T and MGH1138-1 cells, which expressing KRASG12C or KRASG12C/Y96D.
Concentration: 0-100 nM
Incubation Time: 4 hours
Result: Inhibited KRAS, pERK and pRSK levels with similar potency.
Molecular Weight

985.22

Formula

C₅₆H₇₂N₈O₈

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Product Name:
RM-018
Cat. No.:
HY-141477
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