N-{22-ethyl-21-[2-(1-methoxyethyl)pyridin-3-yl]-18,18-dimethyl-9,15-dioxo-16-oxa-10,22,28-triazapentacyclo[18.5.2.12,?.11?,1?.023,2?]nonacosa-1(26),2(29),3,5,20,23(27),24-heptaen-8-yl}-3-methyl-2-(N-methyl-1-{1-[4-(morpholin-4-yl)but-2-ynoyl]pyrrolidin-3-yl}formamido)butanamide

CAS NO.：2641993-55-5
Empirical Formula: C56H72N8O8
Molecular Weight: 985.22
Update Date: 2026-04-24 14:58:24

What is N-{22-ethyl-21-[2-(1-methoxyethyl)pyridin-3-yl]-18,18-dimethyl-9,15-dioxo-16-oxa-10,22,28-triazapentacyclo[18.5.2.12,?.11?,1?.023,2?]nonacosa-1(26),2(29),3,5,20,23(27),24-heptaen-8-yl}-3-methyl-2-(N-methyl-1-{1-[4-(morpholin-4-yl)but-2-ynoyl]pyrrolidin-3-yl}formamido)butanamide?

Biological Activity

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].

References

[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.

Properties of N-{22-ethyl-21-[2-(1-methoxyethyl)pyridin-3-yl]-18,18-dimethyl-9,15-dioxo-16-oxa-10,22,28-triazapentacyclo[18.5.2.12,?.11?,1?.023,2?]nonacosa-1(26),2(29),3,5,20,23(27),24-heptaen-8-yl}-3-methyl-2-(N-methyl-1-{1-[4-(morpholin-4-yl)but-2-ynoyl]pyrrolidin-3-yl}formamido)butanamide

Density	1.27±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
pka	13.44±0.40(Predicted)
form	Solid
color	Off-white to light yellow

Safety information for N-{22-ethyl-21-[2-(1-methoxyethyl)pyridin-3-yl]-18,18-dimethyl-9,15-dioxo-16-oxa-10,22,28-triazapentacyclo[18.5.2.12,?.11?,1?.023,2?]nonacosa-1(26),2(29),3,5,20,23(27),24-heptaen-8-yl}-3-methyl-2-(N-methyl-1-{1-[4-(morpholin-4-yl)but-2-ynoyl]pyrrolidin-3-yl}formamido)butanamide

Computed Descriptors for N-{22-ethyl-21-[2-(1-methoxyethyl)pyridin-3-yl]-18,18-dimethyl-9,15-dioxo-16-oxa-10,22,28-triazapentacyclo[18.5.2.12,?.11?,1?.023,2?]nonacosa-1(26),2(29),3,5,20,23(27),24-heptaen-8-yl}-3-methyl-2-(N-methyl-1-{1-[4-(morpholin-4-yl)but-2-ynoyl]pyrrolidin-3-yl}formamido)butanamide

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