| Hazard Information | Back Directory | [Uses]
BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078))[1]. | [in vivo]
BSJ-5-63 (50 mg/kg; i.p.; daily for 12 days) shows anticancer activity in mice[1]. | Animal Model: | 4-5 weeks, Male ICR-SCID mice (22Rv1 cells)[1] | | Dosage: | 50 mg/kg | | Administration: | I.p.; daily for 12 days | | Result: | Significantly inhibited the growth of 22Rv1 tumors and tumor weight was significantly reduced and increased in the number of apoptotic cells, daily administration resulted in approximately 10% weight loss in mice. |
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CDK12; CDK7; CDK9 | [References]
[1] Gui F, et al. Acute BRCAness Induction and AR Signaling Blockage through CDK12/7/9 Degradation Enhances PARP Inhibitor Sensitivity in Prostate Cancer. bioRxiv [Preprint]. 2024 Jul 10:2024.07.09.602803. DOI:10.1101/2024.07.09.602803 |
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