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AMG-510 (Sotorasib) selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant.
In tumor models, AMG 510 rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. AMG 510 (orally, once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer.
J Immunother Cancer. 2025 Jul 23;13(7):e010514.
Specific inhibitor to KRASG12C induces tumor-specific immunity and synergizes with oncolytic virus for enhanced cancer immunotherapy
AMG-510 purchased from AbMole
iScience. 2023 Jan 28;26(2):106080..
Global profiling of AMG510 modified proteins identified tumor suppressor KEAP1 as an off-target
AMG-510 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | H23 and H358 cell lines |
| Preparation method | To determine the IC50 value of AMG-510 and Cisplatin in H23 and H358 cell lines, we used Cell Count Kit8 after 72 h of drug treatment. In this assay, 3000 cells were seeded on 96-well plates and incubated for cell apposition in their complete medium and subsequently for 72 h with scalar doses of AMG-510 (0–50 µM) or Cisplatin (0–5µM) as single agents or as a constant combination. |
| Concentrations | 0–50 µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Balb/C nude mice |
| Formulation | Dimethyl sulfoxide and H2O |
| Dosages | 30 mg/kg per day |
| Administration | Oral gavage |
| Molecular Weight | 560.59 |
| Formula | C30H30F2N6O3 |
| CAS Number | 2296729-00-3 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] David S Hong, et al. KRAS G12C Inhibition with Sotorasib in Advanced Solid Tumors
[3] No authors listed. Cancer Discov. AMG 510 Shows Activity beyond NSCLC
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