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Inobrodib

CAS No. : 2222941-37⁻⁷

MCE 国际站：Inobrodib

产品活性：Inobrodib (CCS1477) 是一种口服活性的、有效且选择性强的 p300/CBP 抑制剂。Inobrodib 与 p300 和 CBP 结合，K_d 值为 1.3 和 1.7 nM，与 K_d 为 222 nM 的 BRD4 相比，具有 170/130 倍的选择性。Inobrodib 抑制前列腺癌细胞系的细胞增殖并降低雄激素受体 (AR) 和 C-MYC 调节的基因表达。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: Inobrodib binding to cellular histones in an in-cell BRET assay gives an IC50 of 19 nM for p300 and 1,060 nM for BRD4. Inobrodib shows potent growth-inhibitory activity in VCaP, 22Rv1, and LNCaP95 (all IC50 < 100 nM) that express both AR-FL and AR-V7.
Inobrodib (0-3000 nM; 48 hours) reduces expression of AR-regulated genes (KLK2, KLK3, and TMPRSS2) in both 22Rv1 and LNCaP95 cells. Inobrodib also reduces C-MYC protein expression in both 22Rv1 and LNCaP95 cells and AR-V7 protein expression in 22Rv1 cells, without clear impact on AR-FL protein expression in 22Rv1 and LNCaP95 cells. Inobrodib reduces C-MYC mRNA and downstream AR and C-MYC signaling in 22Rv1 and C4-2 cells at 16 hours. Inobrodib regulates AR signaling by affecting the recruitment of CBP, p300, and AR-FL to known AR binding sites, and has the potential to abrogate persistent AR signaling in CRPC.

In Vivo: Inobrodib (10-30 mg/kg; oral gavage; 10 or 20 mg/kg daily (QD) or 30 mg/kg every other day (QOD) for 28 days) suppresses growth of a 22Rv1 mouse xenograft model with associated reduction in AR signaling.
Inobrodib (20 mg/kg; oral gavage; daily for 8 days) decreases AR and AR-V7 signaling and inhibits growth in a patient- derived model of lethal prostate cancer (NOD/SCID gamma (NSG) male castrated mice).

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