PROTAC HSP90 degrader BP3

Name: PROTAC HSP90 degrader BP3
Brand: MedChemExpress
SKU: HY-115997
Rating: 4.5 (1 reviews)

Cat. No.: HY-115997 Purity: 98.56%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2669072-88-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 715	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 715	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1020	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1880	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 4200	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

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

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]

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.

2669072-88-0

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
10 mM	0.1560 mL	0.7799 mL	1.5599 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.

Molarity Calculator
Dilution Calculator

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

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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mg/kg

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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

Purity: 98.56%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (251 KB) HNMR (143 KB) RP-HPLC (256 KB) LCMS (601 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

Complete Stock Solution Preparation Table

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