GDC-0980 (CAS 1032754-93-0)

GDC-0980, also recognized as apitolisib, stands as a potent and selective antagonist for class I PI3K and mTOR kinases, displaying remarkable specificity with a Ki of 17 nM against mTOR (FRAP) and IC50 values of 5 nM, 27 nM, 7 nM, and 14 nM against PI3Kα, β, δ, and γ isoforms, respectively. This small molecule operates by finely tuning the kinase activity central to cellular signaling networks that govern cell proliferation, survival, and angiogenesis, key processes involved in the progression of pathological states. By targeting both PI3K and mTOR pathways, GDC-0980 disrupts the intricate signaling cascades, leading to a marked inhibition of cell proliferation, as evidenced in cancer cell lines like PC3 and MCF7. This dual inhibition strategy offers a comprehensive blockade of the PI3K/AKT/mTOR axis, a pivotal signaling pathway often dysregulated in various conditions, thereby effectively curtailing the aberrant cellular growth and promoting apoptosis without engaging in the complexities of structural breakdown or focusing on clinical applicability. Through these mechanisms, apitolisib exemplifies a strategic approach in research applications to explore the underlying dynamics of cellular growth and survival pathways, contributing valuable insights into the modulation of key molecular drivers of disease progression.