| Bioactivity | CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker)[1]. |
| Invitro | CBPD-268 (4, 24 h) 在 22Rv1 细胞中对 CBP 和 p300 蛋白显示出高降解效率，4 小时时 DC50s 为 0.01、0.03 nM[1].CBPD-268 通过与 CBP/p300 和 CRBN 蛋白结合而显示出降解作用[1]。CBPD-268 (0-1000 nM; 4 days) 抑制细胞生长，对 22Rv1、LNCaP、VCaP 细胞的 IC50 值分别为 3.7、10.3、4.6 nM [1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CBPD-268 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | CBPD-268 (0.3, 1, 3, 10, 30 mg/kg; p.o.; once) 单次口服 0.3-3 mg/kg 可诱导肿瘤组织中 CBP 和 p300 蛋白的降解[1].CBPD-268 (1, 3 mg/kg; p.o.; twice a week for 1 mg/kg or 3 mg/kg weekly for 4-weeks) 显示出抗肿瘤活性[1]。药代动力学分析[1]. Species |
| Formula | C44H47F2N9O5 |
| Molar Mass | 819.90 |
| 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]. Chen Z, et al. Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression. J Med Chem. 2024 Apr 11;67(7):5275-5304. |