RM-018 |
| Catalog No.GC63562 |
Le RM-018 est un inhibiteur À l'état actif puissant et distinct du tricomplexe KRASG12C. RM-018 conserve la capacité de se lier et d'inhiber KRASG12C/Y96D et pourrait surmonter la résistance. RM-018 se lie spécifiquement À l'état actif [\RM-018 binds specifically to the GTP-bound, active ["RAS(ON)"] state of KRASG12C.en_fr_2022q1.md
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Cas No.: 2641993-55-5
Sample solution is provided at 25 µL, 10mM.
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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].
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].
[1]. Tanaka N, et.al. Clinical Acquired Resistance to KRASG12C 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.
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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