RO4929097 is an orally-bioavailable, potent and selective inhibitor of γ-secretase (IC₅₀= 4 nM), producing inhibitory activity of Notch signaling in tumor cells. The potency of RO4929097 in cell-free and cellular assays is in low nanomolar range with >100-fold selectivity with respect to 75 other proteins of various types including receptors, ion channels, and enzymes. RO4929097 does not block tumor cell proliferation or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype. It is currently undergoing phase I dose escalation in patients with solid tumors ^[1-2].

Chemical Properties