PROTAC HSP90 degrader BP3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PROTAC HSP90 degrader BP3 

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 µM)。PROTAC HSP90 degrader BP3 抑制乳腺癌细胞的生长。

PROTAC HSP90 degrader BP3

PROTAC HSP90 degrader BP3 Chemical Structure

CAS No. : 2669072-88-0

规格 价格 是否有货
5 mg ￥6500 询问价格 & 货期
10 mg ￥10200 询问价格 & 货期

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生物活性

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].

IC50 & Target

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)[1].
PROTAC HSP90 degrader BP3 (2 µM; 6 h) shows degradation activity in the MCF-7 cells (DC50=0.99 µM)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

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%[1].

上海金畔生物科技有限公司 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[1]
Dosage: 40 mg/kg
Administration: i.p., daily, 12 days
Result: Inhibited tumor growth and the tumor inhibition rate was 76.41%.

分子量

641.08

Formula

C32H29ClN8O5
CAS 号

2669072-88-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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