No significant accumulation observed after multiple dosing (steady‑state reached by Day 5).
Mukd‑546: Pre‑clinical Evaluation of a Novel Small‑Molecule Inhibitor of the MAPK/ERK Pathway for Targeted Cancer Therapy mukd-546
A. Patel (email: a.patel@cam.ac.uk)
Annexin V‑FITC/PI staining (BD Biosciences) and flow cytometry quantified apoptosis after 48 h treatment (IC₅₀ concentration). Propidium iodide staining after ethanol fixation assessed cell‑cycle distribution. mukd-546
| Cell Line | Mutation | IC₅₀ (nM) | |-----------|----------|-----------| | MIA‑PaCa‑2 | KRAS‑G12C | 45 ± 3 | | PANC‑1 | KRAS‑G12D | 62 ± 5 | | A375 | BRAF‑V600E | 28 ± 2 | | SK‑MEL‑28 | BRAF‑V600E | 32 ± 3 | | A549 | KRAS‑G12S | 78 ± 6 | | HCT‑116 | KRAS‑G13D | 71 ± 5 | | Others (non‑mutated) | – | 210‑480 | mukd-546
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