1. PROTAC Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. PROTACs HSP
  3. PROTAC HSP90 degrader BP3

PROTAC HSP90 degrader BP3 

目录号: HY-115997 纯度: 98.56%
COA 产品使用指南

PROTAC HSP90 degrader BP3 以 CRBN 依赖性方式有效且选择性地降解 HSP90PROTAC 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。

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PROTAC HSP90 degrader BP3 Chemical Structure

PROTAC HSP90 degrader BP3 Chemical Structure

CAS No. : 2669072-88-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥7150
In-stock
1 mg ¥2600
In-stock
5 mg 现货 询价
10 mg   询价  
50 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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 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 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

HSP90

 

Cereblon

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
4T1 IC50
0.61 μM
Compound: 16b; BP3
Anticancer activity against mouse 4T1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Anticancer activity against mouse 4T1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 34864330]
MCF7 IC50
0.63 μM
Compound: 16b; BP3
Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 34864330]
MDA-MB-231 IC50
3.53 μM
Compound: 16b; BP3
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 34864330]
MDA-MB-468 IC50
2.95 μM
Compound: 16b; BP3
Anticancer activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Anticancer activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 34864330]
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].

MCE 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].

MCE 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%.
Clinical Trial
分子量

641.08

Formula

C32H29ClN8O5

CAS 号
性状

固体

颜色

Light yellow to yellow

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
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (155.99 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5599 mL 7.7993 mL 15.5987 mL 38.9967 mL
5 mM 0.3120 mL 1.5599 mL 3.1197 mL 7.7993 mL
10 mM 0.1560 mL 0.7799 mL 1.5599 mL 3.8997 mL
15 mM 0.1040 mL 0.5200 mL 1.0399 mL 2.5998 mL
20 mM 0.0780 mL 0.3900 mL 0.7799 mL 1.9498 mL
25 mM 0.0624 mL 0.3120 mL 0.6239 mL 1.5599 mL
30 mM 0.0520 mL 0.2600 mL 0.5200 mL 1.2999 mL
40 mM 0.0390 mL 0.1950 mL 0.3900 mL 0.9749 mL
50 mM 0.0312 mL 0.1560 mL 0.3120 mL 0.7799 mL
60 mM 0.0260 mL 0.1300 mL 0.2600 mL 0.6499 mL
80 mM 0.0195 mL 0.0975 mL 0.1950 mL 0.4875 mL
100 mM 0.0156 mL 0.0780 mL 0.1560 mL 0.3900 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PROTAC HSP90 degrader BP3
目录号:
HY-115997
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