| Bioactivity | SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis[1]. |
| Invitro | SC912 (0.1-10 μM; 24h) 在 PC3 细胞中有效抑制了 AR 激活，对 GR 和 PR 没有抑制作用 (AR IC50 = 0.57 μM)[1]。SC912 (0.03-100 μM; 1h) 对删除 AR-NTD (氨基酸 507-531) 的 293 T 细胞，与 AR-FL 和 AR-V7 的结合减弱。氨基酸 507-53 1对于对其对抗性活动至关重要[1]。SC912 (2 μM; 24 h） 在 LNCaP95 细胞模型中，强烈抑制了由 AR-V7 唯一调控的 AR 调控基因 (PSA, FKBP5, TMPRSS2) 的转录，表明有效抑制了 AR-V 7介导的转录活性[1]。SC912 (1 μM; 0-24 h）在 LNCaP, VCaP 和 22Rv1 细胞中，引起 G1 期阻滞，引起细胞凋亡[1]。SC912 (3 μM; 5 h） 处理后在 LNCaP 和 LNCaP-AR-V7 细胞中显著减少了 AR-FL 和 AR-V7 的核内积聚，这表明能够有效阻断 AR-V7 的核定位。显著降低了 AR 蛋白与染色质的结合[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> SC912 相关抗体: Apoptosis Analysis[1] Cell Line: |
| In Vivo | SC912 (60 mg/kg; i.p.; 一周五次持续三周) 能有效抑制 VCaP 肿瘤的生长。小鼠的体重没有明显减轻，表明给药剂量具有良好的耐受性[1]。SC912 (90 mg/kg; i.p.; 一周五次持续三周) 即使高度去势抵抗的 22Rv1 模型中，也能减轻肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C22H13Cl2F3N4O2 |
| Molar Mass | 493.27 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Qianhui Y et al. SC912 inhibits AR-V7 activity in castration-resistant prostate cancer by targeting the androgen receptor N-terminal domain Oncogene. 2024 Mar |