Catalog No.: PC-22119Not For Human Use, Lab Use Only.
ORIC-944 (Rinzimetostat) is a potent, selective, allosteric and orally bioavailable PRC2 inhibitor with EED binding EC50 of 106 pM and biochemical PRC2 EC50 of 16.7 nM.
ORIC-944 (Rinzimetostat) is a potent, selective, allosteric and orally bioavailable PRC2 inhibitor with EED binding EC50 of 106 pM and biochemical PRC2 EC50 of 16.7 nM.
ORIC-944 exhibits H3K27me3 IC50 of 26.6 nM in cell based H3K27me3 assay performed in Pfeiffer cells in ELISA format.
ORIC-944 demonstrated single agent tumor growth inhibition in a spectrum of in vivo prostate cancer models, including AR-positive, AR-mutant, ARv7, ARPI-responsive and ARPI-resistant models.
ORIC-944 showed synergy in multiple prostate cancer cells when combined with androgen receptor pathway inhibitors (ARPI).
ORIC-944 inhibits tumor growth and decreases H3K27me3 in prostate cancer xenografts, resulting in increased expression of known PRC2 methylation target genes.
