For research use only. Not for therapeutic Use.
RM-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].
| Catalog Number | I045282 |
| CAS Number | 2641993-55-5 |
| Synonyms | (3S)-N-[(2S)-1-[[(8S,14S)-22-ethyl-21-[2-[(1S)-1-methoxyethyl]pyridin-3-yl]-18,18-dimethyl-9,15-dioxo-16-oxa-10,22,28-triazapentacyclo[18.5.2.12,6.110,14.023,27]nonacosa-1(26),2,4,6(29),20,23(27),24-heptaen-8-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methyl-1-(4-morpholin-4-ylbut-2-ynoyl)pyrrolidine-3-carboxamide |
| Molecular Formula | C56H72N8O8 |
| Purity | ≥95% |
| InChI | InChI=1S/C56H72N8O8/c1-9-63-47-20-19-40-32-43(47)44(51(63)42-16-11-22-57-49(42)37(4)70-8)33-56(5,6)35-72-55(69)45-17-12-24-64(59-45)54(68)46(31-38-14-10-15-39(40)30-38)58-52(66)50(36(2)3)60(7)53(67)41-21-25-62(34-41)48(65)18-13-23-61-26-28-71-29-27-61/h10-11,14-16,19-20,22,30,32,36-37,41,45-46,50,59H,9,12,17,21,23-29,31,33-35H2,1-8H3,(H,58,66)/t37-,41-,45-,46-,50-/m0/s1 |
| InChIKey | KXMPBNBAZLJBDS-GUZCBZAASA-N |
| SMILES | CCN1C2=C3C=C(C=C2)C4=CC=CC(=C4)CC(C(=O)N5CCCC(N5)C(=O)OCC(CC3=C1C6=C(N=CC=C6)C(C)OC)(C)C)NC(=O)C(C(C)C)N(C)C(=O)C7CCN(C7)C(=O)C#CCN8CCOCC8 |
| Reference | [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. |
