Chemical Structure : ORIC-944
CAS No.:
2369769-29-7
ORIC-944
(ORIC944)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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456.53
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Formula
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C26H25FN6O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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8-(4-((dimethylamino)methyl)-2-methylphenyl)-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidine-2-carbonitrile
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References
1. Anneleen Daemen, et al. Cancer Res (2024) 84 (6_Supplement): 6586.
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