| Bioactivity | CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker)[1]. |
| Invitro | CBPD-409 (0.01-10 nM) 抑制前列腺癌细胞 VCaP，LNCaP 和 22Rv1 中的 AR 信号转导和 c-Myc 表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CBPD-409 相关抗体: RT-PCR[1] Cell Line: |
| In Vivo | CBPD-409 (1 mg/kg，静脉注射；3 mg/kg，口服) 在 ICR 小鼠模型中的清除率 CL 为 1.7 mL/min/kg，半衰期为 T1/2 为 2.8 小时 (静脉注射) 和 2.6 小时 (口服)，血药浓度 Cmax 为 2494 ng/mL，口服生物利用度 F=50%[1]。CBPD-409 (0.3-1 mg/kg，口服，每天一次共 5 周) 对 VCaP 前列腺癌具有抗肿瘤活性，肿瘤生长抑制率 TGI 为 73-87%，在 VCaP 异种移植小鼠模型中没有明显毒性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C46H52F2N10O5 |
| Molar Mass | 862.97 |
| 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]. Chen Z, et al., Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer. J Med Chem. 2024 Mar 26. |