ASTX029

ASTX029 (CAS No.: 2095719-92-7) is a synthetic small-molecule protein kinase inhibitor for biomedical research and drug discovery. It is classified as a selective dual inhibitor of extracellular signal-regulated kinases ERK1/2, and is primarily used to elucidate the role of the RAS?RAF?MEK?ERK signaling axis in pathways related to cell proliferation and survival, as well as its pathway dependence in tumor biology. Based on biochemical and cellular profiling assessments, ASTX029 shows high selectivity for ERK kinases, with a reported ERK2 enzymatic inhibition IC50 of approximately 2.7 nM, and can significantly reduce downstream p90 ribosomal S6 kinase (RSK) phosphorylation signals in mutant BRAF- or KRAS-driven models, reflecting consistency with target engagement. In vitro experiments show that it can inhibit cell proliferation in tumor cell lines from multiple origins, including melanoma, colorectal, and lung-derived models, with activity typically observed in the nanomolar to low micromolar range; in established mouse xenograft models, inhibitory effects on tumor growth have been observed, and it has been reported to have oral bioavailability under nonclinical study conditions. ASTX029 is commonly used for target validation of ERK-dependent signaling, studies of pathway regulation and feedback reactivation based on readouts such as phosphorylated RSK, combination screening with inhibitors related to the MAPK pathway, and exploratory pharmacological evaluation in cell and animal models; the specific concentration or dose used in experiments should be determined according to the research objective and experimental design. This product is for laboratory research use only and is not intended for human or veterinary use, clinical application, or any form of ingestion.