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}fo

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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 Suppliers list
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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 Basic information
Product Name: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
Synonyms: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:2641993-55-5
MF:C56H72N8O8
MW:985.22
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Mol File:2641993-55-5.mol
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 Structure
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 Chemical Properties
density 1.27±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
pka13.44±0.40(Predicted)
form Solid
color Off-white to light yellow
Safety Information
MSDS Information
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 Usage And Synthesis
UsesRM-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].
Biological ActivityRM-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].
IC 50KRAS (G12C); KRAS (G12C/Y96D)
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.
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 Preparation Products And Raw materials
Tag: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(2641993-55-5) Related Product Information
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