PROTAC HSP90 degrader BP3
Names
[ CAS No. ]:
2669072-88-0
[ Name ]:
PROTAC HSP90 degrader BP3
Biological Activity
[Description]:
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 (DC50=0.99 µM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell[1].
[Related Catalog]:
[Target]
HSP90
Cereblon
[In Vitro]
PROTAC HSP90 degrader BP3 (compound 16b) (72 h) inhibits the growth of breast cancer cells (IC50=0.63 µM in MCF-7 cells, IC50=3.53 µM in MDA-MB-231 cells, IC50=0.61 µM in 4T1 cells, IC50=2.95 µM in MDA-MB-468 cells)[1]. PROTAC HSP90 degrader BP3 (2 µM; 6 h) shows degradation activity in the MCF-7 cells (DC50=0.99 µM)[1]. Western Blot Analysis[1] Cell Line: MCF-7 cells Concentration: 2 µM Incubation Time: 6 h Result: Showed degradation activity in the MCF-7 cells (DC50=0.99 µM). Cell Viability Assay[1] Cell Line: 4T1, MDA-MB-468 cells Concentration: 0.01, 1, 100, 10000 µM Incubation Time: 72 h Result: Inhibited the growth of cancer cells (IC50=0.61 µM in 4T1 cells, IC50=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%[1]. Animal Model: 6- to 8-week-old female BALB/c mice[1] Dosage: 40 mg/kg Administration: i.p., daily, 12 days Result: Inhibited tumor growth and the tumor inhibition rate was 76.41%.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C32H29ClN8O5
[ Molecular Weight ]:
641.08