PROTAC HSP90 degrader BP3

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2669072-88-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

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。

生物活性

PROTACHSP90 degrader BP3 is a potent and selective degradation ofHSP90in aCRBN-dependent fashion.PROTACHSP90 degrader BP3 has a certain certain degradation effect onHSP90protein in MCF-7 cells (DC₅₀=0.99 μM).PROTACHSP90 degrader BP3 inhibits the growth of breastcancercell^[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].

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].

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%.

Clinical Trial

分子量

641.08

性状

Solid

Formula

C₃₂H₂₉ClN₈O₅

CAS 号

2669072-88-0

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
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL(155.99 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.5599 mL	7.7993 mL	15.5987 mL
5 mM	0.3120 mL	1.5599 mL	3.1197 mL
10 mM	0.1560 mL	0.7799 mL	1.5599 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。