RMC-8839 (RMC8839)

Chemical Structure : RMC-8839

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货号: PC-27075Not For Human Use, Lab Use Only.

RMC-8839 (RMC8839) is a potent, selective, covalent and orally active RAS(ON) G13C tri-complex inhibitor with biochemical Kinact of 2.83 x 10-3 s-1 and Ki of 28.3 nM.

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生物&药学活性

RMC-8839 (RMC8839) is a potent, selective, covalent and orally active RAS(ON) G13C tri-complex inhibitor with biochemical Kinact of 2.83 x 10-3 s-1 and Ki of 28.3 nM.
RMC-8839 inhibits KRASG13C more potently than wild type RAS in a cellular RAS-RAF1 RBD disruption assay, and more potently inhibits pERK and cell proliferation in a cell line harboring a KRASG13C mutation (NCI-H1734) compared to an EGFR-mutant, RASWT cell line (NCI-H1975).
RMC-8839 is 22- to 311-fold selective for KRASG13C over wild-type RAS.
RMC-8839 is ~6x selective for G13C over G12C as this mutation retains a cysteine residue that can be covalently targeted, but is 20 to >100x selective for G13C all other KRAS mutants.
RMC-8839 covalently modifies KRASG13C while retaining the same protein-protein contacts between RAS and CypA.
(100 mg/kg, oral) demonstrated rapid and durable activity achieving tumor target engagement in mice bearing NCI-H1734 (KRASG13C, NSCLC) xenograft tumors, induced RAS-MAPK pathway suppression reached >95%, exhibited great tumor growth inhibition leading to tumor stasis.
Combination of RMC-8839 and RAS(ON) multi-selective inhibitor daraxonrasib resulted in strong pathway suppression and deep and durable tumor regressions in KRASG13C mutant NCI-H1734 xenograft models.

物理化学性质&存储条件

分子量	1032.22
分子式	C54H72F3N9O8
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(4S)-3-acryloyl-N-((2S)-1-(((63S,4S)-12-(2-((S)-1-methoxyethyl)pyridin-3-yl)-10,10-dimethyl-5,7-dioxo-11-(2,2,2-trifluoroethyl)-21,22,23,26,61,62,63,64,65,66-decahydro-11H-8-oxa-1(5,3)-indola-6(1,3)-pyridazina-2(5,1)-pyridinacycloundecaphane-4-yl)amino)-3-methyl-1-oxobutan-2-yl)-N,4-dimethyl-1-oxa-3,8-diazaspiro[4.5]decane-8-carboxamide

参考文献

1. Seamon KJ, et al. Cancer Discov. 2026 Jun 22. doi: 10.1158/2159-8290.CD-25-0886.

2. McDaid WJ, et al. Cancer Discov. 2026 Jun 22. doi: 10.1158/2159-8290.CD-25-0884.

RMC-8839 (RMC8839)

生物&药学活性

物理化学性质&存储条件

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RMC-8839 (RMC8839)

生物&药学活性

物理化学性质&存储条件

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