| Bioactivity | ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer[1]. |
| Invitro | ERα degrader 10（化合物 A20) 对 MCF-7 细胞具有突出的抗增殖作用 (IC50 of 0.28 nM)。ERα degrader 10（化合物 A20；0.1-1000 nM；1-48 h）表现出浓度依赖性 ERα 降解，24 h 降解效果最佳，通过蛋白酶体介导的蛋白质降解途径[1]。ERα degrader 10（10-100 nM；24 h）可抑制 ERα 信号转导，诱导 MCF-7 细胞周期停滞于 G1 期[1]。MCF-7 cells[1]10 nM, 50 nM, 100 nM24 hCould induce cell cycle arrest in G1 phase. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ERα degrader 10 相关抗体: Western Blot Analysis[1] Cell Line: |
| In Vivo | ERα degrader 10（10-30 mg/kg；口服灌胃；每日一次；持续 30 天）在体内 MCF-7 异种移植模型中表现出优异的抗肿瘤作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C29H25ClN2O2 |
| Molar Mass | 468.97 |
| 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]. Rupeng Dai, et al. Drug discovery of N-methyl-pyrazole derivatives as potent selective estrogen receptor degrader (SERD) for the treatment of breast cancer. Eur J Med Chem. 2024 Sep 23:279:116894. |