PROTAC HSP90 degrader BP3 以 CRBN 依赖性方式有效且选择性地降解 HSP90。PROTAC HSP90 degrader BP3对 MCF-7 细胞中的 HSP90 蛋白有一定的降解作用 (DC50=0.99 ?M)。PROTAC HSP90 degrader BP3 抑制乳腺癌细胞的生长。
货号:ajcx38370
CAS:2669072-88-0
分子式:C32H29ClN8O5
分子量：641.08
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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].

[1]. Liu Q, et al. Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer. Eur J Med Chem. 2022, 228:114013.