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Chemical Structure : ORIC-944
Catalog No.: PC-22119Not For Human Use, Lab Use Only.
ORIC-944 (ORIC944) 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.
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ORIC-944 (ORIC944) 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.
| M.Wt | 456.53 | |
| Formula | C26H25FN6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Anneleen Daemen, et al. Cancer Res (2024) 84 (6_Supplement): 6586.
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