| Bioactivity | WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4[1]. |
| Invitro | WWL0245 (0-1 μM; 96h) 抑制 AR 阳性前列腺癌细胞的增殖，IC50值范围为 0.0159 μM ~ 10 μM。在 [1]时，对 AR 阳性细胞株 VCaP、LNCaP、22Rv1 表现出较强的抗增殖活性, IC50 值分别为 0.016 μM、0.021 μM、0.053 μM。WWL0245 (1 μM; 24 h) 导致 LNCaP、22Rv1、VCaP 细胞系 BRD4 和 c-Myc 呈时间依赖性下调，导致 22Rv1 和 VCaP 细胞 BRD4 水平和 c-Myc 水平呈浓度依赖性降低。WWL0245 也可以下调 DU145 细胞中的 BRD4 水平，但对 c-Myc 水平的影响可以忽略不计[1]。WWL0245 (100 nM-1 μM; 24小时) 不同程度地抑制 AR 调控基因 (PSA、TMPRSS2、ERG、FKBP5、BMPR1B) 的转录[1]。 Cell Proliferation Assay[1] Cell Line: |
| Name | WWL0245 |
| CAS | 2869057-11-2 |
| Formula | C45H51N11O8 |
| Molar Mass | 873.96 |
| 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]. Rong Hu, et al. Identification of a selective BRD4 PROTAC with potent antiproliferative effects in AR-positive prostate cancer based on a dual BET/PLK1 inhibitor. Eur J Med Chem. 2022 Jan 5;227:113922. |