Avapritinib (BLU-285)

Avapritinib (BLU-285) (CAS No.: 1703793-34-3) is a synthetic small molecule kinase inhibitor in the targeted signaling modulator category that is widely used as a biochemical and pharmacology research tool for oncology focused pathway interrogation, with primary activity against activation loop mutant forms of KIT and PDGFRA and additional reported modulation of ABC transporter function, including attenuation of ABCB1 and ABCG2 mediated transport in experimental systems; mechanistically, it is characterized by high selectivity and potent inhibition of mutant kinase signaling through interaction with catalytically active kinase conformations, leading to suppression of downstream phosphorylation dependent proliferative signaling networks relevant to mutant receptor tyrosine kinase biology, and published in vitro findings place its inhibitory potency in the nanomolar range for key mutant targets such as KIT D816V and PDGFRA D842V, while cellular pathway suppression is generally observed from nanomolar to low micromolar conditions depending on model context, assay format, exposure duration, and endpoint selection; in biomedical research and discovery workflows, this compound is commonly applied in engineered cell lines, patient derived cellular systems, and xenograft or other preclinical animal models to study mutant kinase dependency, resistance mechanisms, transporter associated compound disposition, and combination strategy hypotheses, and the concentrations or doses used in experiments typically depend on specific experimental designs and research objectives, including target expression level, mutation status, pharmacodynamic biomarkers, and tolerability constraints within nonclinical study frameworks.