Cat. No.: HY-155113

PROTAC Hsp90α degrader 1

Customer Review

Based on 1 Customer Validation

PROTAC Hsp90α degrader 1 is a selective PROTAC Hsp90α degrader with a DC₅₀ of 0.295 μM. PROTAC Hsp90α degrader 1 exhibits antitumor activity with low toxic side effects. PROTAC Hsp90α degrader 1 can be used for the research of breast cancer.
(Pink: HSP90α Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker).

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

Purity: 98.30%
CAS No.: 3031078-90-4
Formula: C₄₃H₅₀N₆O₇
Molecular Weight:762.89

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PROTAC Hsp90α degrader 1 Chemical Structure

CAS No.: 3031078-90-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC Hsp90α degrader 1 is a selective PROTAC Hsp90α degrader with a DC₅₀ of 0.295 μM. PROTAC Hsp90α degrader 1 exhibits antitumor activity with low toxic side effects. PROTAC Hsp90α degrader 1 can be used for the research of breast cancer^[1]. (Pink: HSP90α Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker).

IC₅₀ & Target^[1]

HSP90α

0.295 μM (DC₅₀)

All PROTACs Isoforms :

All HSP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	8.93 μM Compound: X10g	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 37619298]
MDA-MB-231	IC₅₀	51.48 μM Compound: X10g	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: 37619298]
MDA-MB-468	IC₅₀	16.46 μM Compound: X10g	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 37619298]
MX1	IC₅₀	11.95 μM Compound: X10g	Antiproliferative activity against human MX1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MX1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 37619298]

In Vitro

PROTAC Hsp90α degrader 1 (compound X10g) (72 h) inhibits proliferation of MDA-MB-231, MDA-MB-468, MCF-7, and MX-1 breast cancer cell lines with IC₅₀ values of 51.48, 16.46, 8.93, and 11.95 μM, respectively^[1].
PROTAC Hsp90α degrader 1 directly binds to both Hsp90α and CRBN to form a stable ternary complex^[1].
PROTAC Hsp90α degrader 1 (0.1-5 μM; 4-8 h) selectively degrades Hsp90α in MCF-7 cells in a dose- and time-dependent manner^[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 breast cancer cells
Concentration:

0.1; 0.2; 0.5; 1; 2; 5 μM
Incubation Time:

4; 6; 8 h
Result:

Selectively degraded Hsp90α but not Hsp90β at 0.5 μM for 8 h.
Showed a maximum Hsp90α degradation ratio (Dmax) of 66.4%, with a hook effect observed at high concentrations.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_all	AUC_inf	MRT	T_1/2
Rat^[1]	15 mg/kg	i.p.	36 min	302 ng/mL	42207 min·ng/mL	45479 min·ng/mL	167 min	150 min

In Vivo

PROTAC Hsp90α degrader 1 (60 mg/kg; i.p.; daily; 20 days) exhibits potent antitumour activity in mouse 4T-1 xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c mice (female; bearing 4T-1 tumour xenografts)^[1]
Dosage:

60 mg/kg
Administration:

i.p.; daily; 20 days
Result:

Achieved a tumour inhibition rate of 53.99%.
Reduced tumour weights significantly compared to control groups.
Maintained stable mouse body weights throughout the treatment period.
Caused no deaths in the treatment group.

Chemical Information

CAS No. 3031078-90-4
Appearance Solid
Molecular Weight 762.89
Formula C₄₃H₅₀N₆O₇
Color White to off-white
SMILES

OC1=CC=C(C(N2CC3=CC=C(CN4CCN(CCCCCCC(NC5=C6C(C(N(C7C(NC(CC7)=O)=O)C6=O)=O)=CC=C5)=O)CC4)C=C3C2)=O)C=C1C(C)C
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 (131.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3108 mL

6.5540 mL

13.1080 mL

5 mM

0.2622 mL

1.3108 mL

2.6216 mL

10 mM

0.1311 mL

0.6554 mL

1.3108 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jiang Q, et al. Discovery of X10g as a selective PROTAC degrader of Hsp90α protein for treating breast cancer. Eur J Med Chem. 2023;260:115690. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.3108 mL	6.5540 mL	13.1080 mL	32.7701 mL
	5 mM	0.2622 mL	1.3108 mL	2.6216 mL	6.5540 mL
	10 mM	0.1311 mL	0.6554 mL	1.3108 mL	3.2770 mL
	15 mM	0.0874 mL	0.4369 mL	0.8739 mL	2.1847 mL
	20 mM	0.0655 mL	0.3277 mL	0.6554 mL	1.6385 mL
	25 mM	0.0524 mL	0.2622 mL	0.5243 mL	1.3108 mL
	30 mM	0.0437 mL	0.2185 mL	0.4369 mL	1.0923 mL
	40 mM	0.0328 mL	0.1639 mL	0.3277 mL	0.8193 mL
	50 mM	0.0262 mL	0.1311 mL	0.2622 mL	0.6554 mL
	60 mM	0.0218 mL	0.1092 mL	0.2185 mL	0.5462 mL
	80 mM	0.0164 mL	0.0819 mL	0.1639 mL	0.4096 mL
	100 mM	0.0131 mL	0.0655 mL	0.1311 mL	0.3277 mL

Keywords

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PROTAC Hsp90α degrader 1

Bioactive Compound Library Max

Bioactive Compound Library

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Metabolic Enzyme Compound Library

PROTAC Library

Extracellular Vesicles (EVs) Compound Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

All PROTACs Isoforms

All HSP Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PROTAC Hsp90α degrader 1

Bioactive Compound Library Max

Bioactive Compound Library

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Metabolic Enzyme Compound Library

PROTAC Library

Extracellular Vesicles (EVs) Compound Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

All PROTACs Isoforms

All HSP Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PROTAC Hsp90α degrader 1 Related Classifications

HY-155113 Related Classifications