ORIC-944 | PRC2 inhibitor | Probechem Biochemicals

Chemical Structure : ORIC-944

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ORIC-944 (ORIC944)

货号: 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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25 mg		Get quote
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250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	456.53
分子式	C26H25FN6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	8-(4-((dimethylamino)methyl)-2-methylphenyl)-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidine-2-carbonitrile

参考文献

1. Anneleen Daemen, et al. Cancer Res (2024) 84 (6_Supplement): 6586.

ORIC-944 (ORIC944)

生物&药学活性

物理化学性质&存储条件

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ORIC-944 (ORIC944)

生物&药学活性

物理化学性质&存储条件

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