2641993-55-5
2641993-55-5 structure
- Name: RM-018
- Chemical Name: RM-018
- CAS Number: 2641993-55-5
- Molecular Formula: C56H72N8O8
- Molecular Weight: 985.22
- Catalog: Signaling Pathways GPCR/G Protein Ras
- Create Date: 2022-01-19 18:12:15
- Modify Date: 2024-01-11 17:52:39
-
RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retaines 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].
| Name | RM-018 |
|---|
| Description | RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retaines 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]. |
|---|---|
| Related Catalog | |
| Target |
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 an IC50 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 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. |
| References |
| Molecular Formula | C56H72N8O8 |
|---|---|
| Molecular Weight | 985.22 |