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Chemical Structure : RMC-6291
CAS No.: 2641998-63-0
Catalog No.: PC-20608Not For Human Use, Lab Use Only.
RMC-6291 (RMC6291) is a potent, covalent, next-generation, mutant-selective inhibitor of active state KRAS G12C(ON) with IC50 of 0.7 nM (pERK), RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $458 | In stock | |
| 5 mg | $758 | In stock | |
| 10 mg | $1180 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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RMC-6291 (RMC6291) is a potent, covalent, next-generation, mutant-selective inhibitor of active state KRAS G12C(ON) with IC50 of 0.7 nM (pERK), RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA).
RMC-6291 potently inhibits HCI-H358 cell growth (KRAS G12C) with IC50 of 0.09 nM, >10000-fold selectivity over WT cell.
RMC-6291 overcomes the limitations of first-generation KRASG12C(OFF) inhibitors in preclinical models by directly targeting the active form of KRAS G12C.
Oral administration of RMC-6291 produces deep and durable suppression of RAS pathway activity in KRASG12C tumor models and drives profound tumor regressions in vivo at well-tolerated doses.
RMC-6291 outperforms MRTX849 (Adagrasib, Cat. PC-72227), a KRASG12C(OFF) inhibitor, in mouse clinical trial consisting of multiple patient- and cell line-derived xenograft models of KRASG12C NSCLC.
Combination treatment with RMC-6291 and SHP2 or SOS1 inhibitors was well tolerated in preclinical models and further increased anti-tumor activity.
RMC-6291 also combined well with immune checkpoint inhibitors, sensitizing KRASG12C-bearing cancer models to anti-tumor immunity.
| M.Wt | 1012.28 | |
| Formula | C55H78FN9O8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
C[C@H](OC)C(N=CC=C1)=[C@@]1[C@](N2CC)=C(CC(C)(C)COC([C@H]3NN(C([C@@H](NC([C@H](C(C)C)N(C(C4(F)CCN(C(C#CC(N(C)C)(C)C)=O)CC4)=O)C)=O)C[C@H]5CN6CCO5)=O)CCC3)=O)C7=C2C=CC6=C7 |
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1. Robert J. Nichols, et al. Cancer Res (2022) 82 (12_Supplement): 3595.
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