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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-ORIC-944
ORIC-944

Chemical Structure : ORIC-944

CAS No.: 2369769-29-7

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ORIC-944 (Rinzimetostat, ORIC944)

货号: 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.

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

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.

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