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.
性状
Solid
IC50 & Target[1][2]
HSP90 Cereblon
体外研究(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).PROTAC HSP90 degrader BP3 (2 μM; 6 h) shows degradation activity in the MCF-7 cells (DC50=0.99 μM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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%. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: 6- to 8-we
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (155.99 mM; Need ultrasonic)配制储备液