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SC912

CAS No. :

MCE 站：SC912

产品活性：:SC912 是一种AR-V7(IC₅₀ = 0.36 μM) 抑制剂，拥有安全性，高效性和选择性，直接和 AR-FL 和 AR-V7 蛋白结合，抑制了核定位和染色质结合能力。通过抑制增殖，诱导细胞周期停止和凋亡来发挥抗癌活性。

研究领域：Vitamin D Related/Nuclear Receptor  |  Apoptosis

作用靶点：Androgen Receptor  |  Apoptosis

In Vitro: SC912 (0.1-10 μM; 24 h) effectively inhibits AR activation in PC3 Cells. No inhibition of GR ａnd PR (AR IC₅₀ = 0.57 μM).
SC912 (0.03-100 μM; 1 h) binding to AR-FL ａnd AR-V7 is attenuated in 293 T cells deleted for AR-NTD amino acids 507-531. Amino acids 507-531 are essential for the antagonistic activity.
SC912 (2 μM; 24 h) strongly represses the transcription of AR-regulated genes (PSA, FKBP5, TMPRSS2) that are uniquely regulated by AR-V7 in the LNCaP95 cell model, suggesting effective repression of AR-V7-mediated transcriptional activity.
SC912 (1 μM; 24 h) leads to G1 phase blockade ａnd causes apoptosis in LNCaP, VCaP ａnd 22Rv1 cells.
SC912 (3 μM; 5 h) significantly reduces the intranuclear accumulation of AR-FL ａnd AR-V7 in LNCaP ａnd LNCaP-AR-V7 cells, suggesting that is able to effectively block the nuclear localization of AR-V7. SC912 also significantly reducs the binding of AR proteins to the chromatin.

In Vivo: SC912 (60 mg/kg; i.p.;5 times days for 3 weeks) halts the growth of VCaP tumors effectively. No noticeable loss in body weight of the mice, indicating good tolerability at the administered dose.
SC912 (90 mg/kg; i.p.; 5 days a week for 3 weeks) alleviates tumor progression even in this highly castration-resistant 22Rv1 model.

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