2642037-07-6
Chemical Structure
RMC-4998
- CAS No.: 2642037-07-6
- Formula:C57H74N8O7
- Molecular Weight:983.25
InChIKey: VYZILERTWJIGRC-DOESOIHZSA-N
SMILES: O=C(N1CCC[C@@H](C2=O)N1)[C@@H](NC([C@H](C(C)C)N3C([C@@]4(CCN(C(C#CC(C)(C)N(C)C)=O)C4)CC3)=O)=O)CC5=CC(C6=CC(C(CC(C)(C)CO2)=[C@@]([C@@]7=C([C@H](C)OC)N=CC=C7)N8CC)=C8C=C6)=CC=C5
Biological Activity: RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research[1][2].
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RMC-4998 | 99.31% | RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research. | ||||||||||||||||||||
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References
- [1]. Schulze CJ, et al. Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS. Science. 2023 Aug 18;381(6659):794-799. [Content Brief]
- [2]. Kitai H,et al. Combined inhibition of KRASG12C and mTORC1 kinase is synergistic in non-small cell lung cancer. Nat Commun. 2024 Jul 19;15(1):6076. [Content Brief]
