The preclinical pharmacokinetics of Tolinapant-A dual cIAP1/XIAP antagonist with in vivo efficacy.
Pharmacology research & perspectives • Vol. 12, Issue 6 • 2024
Novel smac mimetic ASTX660 (Tolinapant) and TNF-α synergistically induce necroptosis in bladder cancer cells in vitro upon apoptosis inhibition.
Biochemical and biophysical research communications • Vol. 602 • 2022
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).
Journal of medicinal chemistry • Vol. 61, Issue 16 • 2018
ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth.
Molecular cancer therapeutics • Vol. 17, Issue 7 • 2018
