ASTX029 (Example 1) is a highly potent dual inhibitor of ERK1 and ERK2, with an IC₅₀ of 2.7 nM. By directly targeting both isoforms of extracellular signal-regulated kinase, ASTX029 effectively blocks downstream MAPK/ERK signaling, a pathway frequently dysregulated in cancer. It exhibits strong anticancer activity and is being investigated as a therapeutic candidate for malignancies driven by aberrant RAS-RAF-MEK-ERK signaling.
ASTX029 (Example 1) is a highly potent dual inhibitor of ERK1 and ERK2, with an IC₅₀ of 2.7 nM. By directly targeting both isoforms of extracellular signal-regulated kinase, ASTX029 effectively blocks downstream MAPK/ERK signaling, a pathway frequently dysregulated in cancer. It exhibits strong anticancer activity and is being investigated as a therapeutic candidate for malignancies driven by aberrant RAS-RAF-MEK-ERK signaling.
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 1 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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