Catalog No.: PC-26761Not For Human Use, Lab Use Only.
FORX-428 (FORX428) is a highly potent, selective and orally bioavailable PARG inhibitor with IC50 of 0.29 nM and 0.25 nM for PARG WT human and PARG WT mouse respectively.
FORX-428 (FORX428) is a highly potent, selective and orally bioavailable PARG inhibitor with IC50 of 0.29 nM and 0.25 nM for PARG WT human and PARG WT mouse respectively.
FORX-428 shows high binding affinitt to PARG with SPR Kd of 0.09 nM.
FORX-428 shows selective reduction of viability in a panel of cancer cell lines, RMUG-S (ovarian, IC50=0.6 nM), MDA-MB-436 (breast, IC50=19 nM).
FORX-428 induces a dose-dependent accumulation of PAR chains in vivo which constitutes a tractable target engagement biomarker for clinical exploration.
FORX-428 demonstrates compelling anti-tumor efficacy as single agent in several xenograft models (breast & ovarian cancer) with excellent tolerability.
