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Chemical Structure : RMC-4998
Catalog No.: PC-21063Not For Human Use, Lab Use Only.
RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.
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RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.
RMC-4998 exhibits greater binding affinity (inhibition constant (KI): 272,000 M−1 s−1 (kinact/KI): 272,000 M−1s−1]) than that of existing inactive state-selective inhibitors.
RMC-4998 induces a tricomplex between KRASG12C and CYPA in live cells without affecting wild-type KRAS, NRAS, or HRAS.
RMC-4998 shows comparable activity on G12C-mutant HRAS, NRAS, and KRAS, with little, if any, activity on KRASG13C.
RMC-4998 (0.1 μM) led to a faster disruption of the interaction between KRASG12C and CRAF compared with inactive state-selective inhibitors adagrasib (1 μM) and sotorasib (10 μM) in mutant KRAS in cancer cells.
RMC-4998 inhibits KRASG12C-driven tumor growth in vivo.
| M.Wt | 936.17 | |
| Formula | C51H69N9O8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Christopher J Schulze, et al. Science. 2023 Aug 18;381(6659):794-799.
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