PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN -dependent fashion. PROTAC HSP90 degrader BP3 has a certain certain degradation effect on HSP90 protein in MCF-7 cells ( DC 50 =0.99 µM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell
In Vitro
PROTAC HSP90 degrader BP3 (compound 16b) (72 h) inhibits the growth of breast cancer cells (IC 50 =0.63 µM in MCF-7 cells, IC 50 =3.53 µM in MDA-MB-231 cells, IC 50 =0.61 µM in 4T1 cells, IC 50 =2.95 µM in MDA-MB-468 cells). PROTAC HSP90 degrader BP3 (2 µM; 6 h) shows degradation activity in the MCF-7 cells (DC 50 =0.99 µM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MCF-7 cells Concentration: 2 µM Incubation Time: 6 h Result: Showed degradation activity in the MCF-7 cells (DC 50 =0.99 µM). Cell Viability AssayCell Line: 4T1, MDA-MB-468 cells Concentration: 0.01, 1, 100, 10000 µM Incubation Time: 72 h Result: Inhibited the growth of cancer cells (IC 50 =0.61 µM in 4T1 cells, IC 50 =2.95 µM in MDA-MB-468 cells).
In Vivo
PROTAC HSP90 degrader BP3 (40 mg/kg; i.p., daily for 12 days) inhibits tumor growth and the tumor inhibition rate is 76.41% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6- to 8-week-old female BALB/c mice Dosage: 40 mg/kg Administration: i.p., daily, 12 days Result: Inhibited tumor growth and the tumor inhibition rate was 76.41%.
