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RMC-7977 is a highly selective, reversible, tri-complex RAS inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS, with affinity for both mutant and wild type (WT) variants. RMC-7977 demonstrated potent activity against RAS-addicted tumours carrying various RAS genotypes, particularly against cancer models with KRAS codon 12 mutations (KRASG12X). Treatment with RMC-7977 led to tumour regression and was well tolerated in diverse RAS-addicted cancer models. Additionally, RMC-7977 inhibited the growth of KRASG12C cancer models that are resistant to KRAS(G12C) inhibitors owing to restoration of RAS pathway signalling.
| Cell Experiment | |
|---|---|
| Cell lines | RAS-less mouse embryonic fibroblasts (MEFs) introduced with exogenous wild-type or mutant KRAS genes (KRASG12V, KRASG12D, KRASG12C) or BRAF(V600E) |
| Preparation method | RAS-less MEFs were introduced with exogenous wild-type or mutant KRAS genes or BRAF(V600E). Cells were treated with RMC-7977 at varying concentrations for 24 hours. Western blot analysis was performed to assess pERK suppression. For cell proliferation assays, a panel of 183 cancer cell lines was screened. Cells were cultured in methylcellulose and treated in triplicates with serial dilutions of RMC-7977 (top concentration of 1 µM) or DMSO dispensed by a Tecan D300e digital dispenser. Cells were incubated for 120 h, and cell viability was determined according to the manufacturer's instructions. |
| Concentrations | 3, 10, 30, 100, 300 nM |
| Incubation time | 24 h (Western blot); 120 h (cell viability/proliferation assays) |
| Animal Experiment | |
|---|---|
| Animal models | Subcutaneously implanted NCI-H441 CDX model of non-small cell lung cancer (NSCLC, KRASG12V) in BALB/c mice |
| Formulation | 10% DMSO, 20% PEG 400, 10% Solutol HS15, and 60% water by volume (for in vivo study) |
| Dosages | 10 mg/kg (standard dose); 10, 25, 50 mg/kg (single dose pharmacokinetic study in Capan-1 model) |
| Administration | Oral gavage (p.o.), once daily for 5 days, followed by a 2-day break, totally for 28 days (NCI-H441 model) |
| Molecular Weight | 865.09 |
| Formula | C47H60N8O6S |
| CAS Number | 2765082-12-8 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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