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

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. 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.

For research use only. We do not sell to patients.

PROTAC HSP90 degrader BP3 Chemical Structure

PROTAC HSP90 degrader BP3 Chemical Structure

CAS No. : 2669072-88-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 715 In-stock
Solution
10 mM * 1 mL in DMSO USD 715 In-stock
Solid
5 mg USD 650 In-stock
10 mg USD 1020 In-stock
25 mg USD 1880 In-stock
50 mg USD 2850 In-stock
100 mg USD 4200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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

 

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].

MedChemExpress (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).
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].

MedChemExpress (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
Molecular Weight

641.08

Formula

C32H29ClN8O5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCC#CC4=CN(CC5=NC=C(C)C(OC)=C5C)C6=NC(N)=NC(Cl)=C64)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (155.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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PROTAC HSP90 degrader BP3 Related Classifications

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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Product Name:
PROTAC HSP90 degrader BP3
Cat. No.:
HY-115997
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