RMC-4998 is a tri-complex inhibitor and KRASG12C inhibitor. RMC-4998 targets the active or GTP-bound state of KRASG12C. Disruption of effector binding by RMC-4998 inhibited downstream ERK signaling in KRASG12C mutant cancer cell models with an IC50 ranging between 1 and 10 nM. RMC-4998 had median IC50 of 0.28 nM and selectivity index of 1450. Of note, both the potency and the selectivity index of RMC-4998 and RMC-6291 were greater than those of adagrasib.
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名称 | RMC-4998 |
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Iupac 化学名称 | (2S)-2-((S)-7-(4-(dimethylamino)-4-methylpent-2-ynoyl)-1-oxo-2,7-diazaspiro[4.4]nonan-2-yl)-N-((63S,4S)-11-ethyl-12-(2-((S)-1-methoxyethyl)pyridin-3-yl)-10,10-dimethyl-5,7-dioxo-61,62,63,64,65,66-hexahydro-11H-8-oxa-1(5,3)-indola-6(1,3)-pyridazina-2(1,3)-benzenacycloundecaphane-4-yl)-3-methylbutanamide |
同义词 | RMC-4998; RMC 4998; RMC4998; |
英文同义词 | RMC-4998; RMC 4998; RMC4998; |
分子式 | C57H74N8O7 |
分子量 | 983.268 |
Smile | 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 |
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InChi | |
Cas号 | 2642037-07-6 |
相关CAS号 |
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