PROTAC HSP90 degrader BP3 |
| رقم الكتالوجGC64825 |
PROTAC HSP90 degrader BP3 هو تدهور فعال وانتقائي لـ HSP90 بطريقة تعتمد على CRBNPROTAC HSP90 degrader BP3 له تأثير تدهور معين على بروتين HSP90 في خلايا MCF-7 (DC50 = 0.99 ميكرومتر)يمنع PROTAC HSP90 degrader BP3 نمو خلايا سرطان الثدي
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Cas No.: 2669072-88-0
Sample solution is provided at 25 µL, 10mM.
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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.
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