Catalog No.: PC-21298Not For Human Use, Lab Use Only.
RLY-2608 (RLY2608) is a first-in-class, allosteric, mutant-selective inhibitor of PI3Kα with IC50 of 4 nM (PI3Kα H1047R), 12-fold selective over PI3Kα WT.
RLY-2608 (RLY2608) is a first-in-class, allosteric, mutant-selective inhibitor of PI3Kα with IC50 of 4 nM (PI3Kα H1047R), 12-fold selective over PI3Kα WT.
RLY-2608 is active in cells against tail and helical domain PIK3CA mutations.
RLY-2608 is highly selective over PI3K isoforms and does not detectibly inhibit other kinases.
RLY-2608 (100 mg/kg) inhibits tumors in animal models with reduced impact on insulin levels.
RLY-2608 can maximally inhibit tumors driven by mutations impacting the regulation of PI3Kα while mitigating the hyperglycemia adverse effect that result from inhibiting WT protein.
