| Bioactivity | SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1[1]. | ||||||||||||
| Invitro | SC428 (10 nmol/L- 1μmol/L, 48 h) 在 293T 细胞 (PSA-Luc 实验) 中抑制 AR-V7 (IC50为 0.42 μM) 和 ARv567es (IC50为 1.31 μM) 反式激活活性。SC428 (5μM, 1 h) 在 LNCaP 细胞 (CETSA 实验) 中逆转 DHT 诱导的 AR-FL 热稳定 (EC50为 0.31 μM)，SC428 以浓度依赖的方式抑制配体诱导的 AR 的激活，是 F887 L 突变体的拮抗剂[1]。SC428 (1, 2.5 and 5 μmol/L, 30 min) 抑制 LNCaP (IC50为 1.39 μM)，VCaP (IC50为 1.01 μM)， 22Rv1 (IC50为 1.13 μM) AR 阳性细胞系的增殖。AR 阴性细胞株 PC3 (IC50为 6.49 μM) 中抗增殖能力较弱 [1]。SC428 (5 μmol/L, 5 h) 可减弱LNCaP-AR 细胞 (ChIP 实验) AR 调控基因的转录，阻断AR-FL染色质结合 (共聚焦成像实验)，减少核易位[1]。SC428 (2.5, 5 μmol/L, 24 h) 抑制高表达 AR- V7 前列腺癌细胞的 AR 信号传导 (qPCR 实验)。SC428 (0.5, 1, 2.5 and 5 μmol/L, 24 h) 对 LNCaP-ARV7 和 LNCaP-ARwt 细胞都有抑制效果 (Enzalutamide (HY-70002) - resistant)，蛋白和 mRNA 水平上抑制 PSA 和 UBE2C (蛋白免疫印迹和 qPCR)[1]。SC428 (5 mmol/L, 5h) 在 22Rv1 细胞中破坏 AR-V7 二聚体 (免疫沉淀实验) 和核定位 (共聚焦成像技术)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> SC428 相关抗体: Real Time qPCR[1] Cell Line: | ||||||||||||
| In Vivo | SC428 (60 mg/kg; 腹腔注射; 每天一次; 18天) 在通过体内诱导 AR-V7 肿瘤细胞凋亡抑制肿瘤生长[1]。SC428 (90 mg/kg; 腹腔注射; 每周五次; 3周) 在小鼠体内抑制高表达 AR-V7 的前列腺癌异种移植物的生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
| CAS | 1898232-70-6 | ||||||||||||
| Formula | C15H10F3N3OS | ||||||||||||
| Molar Mass | 337.32 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Qianhui Yi , et al. Discovery of a Small-Molecule Inhibitor Targeting the Androgen Receptor N-Terminal Domain for Castration-Resistant Prostate Cancer. 2023 May 4;22(5):570-582. |