Art. -Nr.: HY-156698

HJM-561

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HJM-561 is a selective and effective orally active EGFR PROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772). HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC₅₀: 9.2 nM) and L858R/T790M/C797S (DC₅₀: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857); blue: CRBN ligand (HY-A0003); black: linker).

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Reinheit: 99.26%
CAS. Nr.: 2570251-68-0
Formel: C₄₅H₅₁ClN₉O₅P
Molecular Weight:864.37

Speicherung:

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

HJM-561 Chemical Structure

CAS. Nr.: 2570251-68-0

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle EGFR Isoform-spezifische Produkte anzeigen :

In Vitro

HJM-561 (0-300 nM, 24 h) potently degrades EGFR Del19/T790M/C797S (DC₅₀: 9.2 nM) and L858R/T790M/C797S (DC₅₀: 5.8 nM), but has no effect on wild-type EGFR^[1].
HJM-561 (100 nM, 24 h) degrades the EGFR triple mutant in Del19/T790M/C797S Ba/F3 cells by activating CRBN E3 ligase and ubiquitin-proteasome system^[1].
EGFR mutant, with IC₅₀ of 15.6 and 17.0 nM in Del19/T790M/C797S cells and L858R/T790M/C797S cells, respectively^[1].
EGFR expression (HEK293T and MDA-MB-231), indicating that it has no effect on cells expressing wild-type EGFR^[1].

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

Western Blot Analysis^[1]

Cell Line:

Del19/T790M/C797S-Ba/F3 cells
Concentration:

100 nM
Incubation Time:

24 h
Result:

Totally rescued EGFR degradation when Del19/T790M/C797S Ba/F3 cells were cotreated with the ubiquitination inhibitor MLN4924 (1 μM).
Failed to induce EGFR degradation in the presence of Pomalidomide (10 μM) in a competitive assay with the cereblon (CRBN) ligand.

Parmacokinetics

Species	Dose	Route	T_1/2	Plasma Concentration	AUC	MRT	Bioavailability
Mice^[1]	1 mg/kg	i.v.	2.42 h	2054.53 ng·h/mL	3135.27 ng·h/mL	1.83 h	/
Mice^[1]	10 mg/kg	p.o.	2.08 h	3677.25 ng/mL	19689.35 ng·h/mL	3.71 h	62.80 %

In Vivo

HJM-561 (20, 40 mg/kg, p.o., once a day for 18 consecutive days) significantly reduces tumor volume by 58% and 84% at 20 mg/kg and 40 mg/kg in the EGFR Del19/T790M/C797S mouse model, and there is no significant change in mouse body weight^[1].
HJM-561 (20, 40 mg/kg, p.o., once a day for 18 consecutive days) dose-dependently inhibits tumor growth in the human xenograft tumor (PDX) model, with a TGI of 67% at a dose of 40 mg/kg, and there is no significant change in mouse body weight^[1].

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

Animal Model:

0.5 million EGFR Del19/T790M/C797S Ba/F3 cells and 50% Matrigel gel were subcutaneously inoculated in Balb/c nude mice (female aged 6-8 weeks)^[1]
Dosage:

20, 40 mg/kg
Administration:

p.o., once a day for 18 consecutive days
Result:

Significantly reduced tumor volume by 58% and 84% at doses of 20 mg/kg and 40 mg/kg.
Showed that EGFR degradation and phosphorylated EGFR inhibition.

Chemical Information

CAS. Nr. 2570251-68-0
Appearance Solid
Molecular Weight 864.37
Formel C₄₅H₅₁ClN₉O₅P
Color Off-white to light yellow
SMILES

O=C1C2=C(CN1C3C(NC(CC3)=O)=O)C(C#CCCN4CCN(C5CCN(CC5)C6=CC=C(C(OC)=C6)NC7=NC=C(C(NC8=C(P(C)(C)=O)C=CC=C8)=N7)Cl)CC4)=CC=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (115.69 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

1.1569 mL

5.7846 mL

11.5691 mL

5 mM

0.2314 mL

1.1569 mL

2.3138 mL

10 mM

0.1157 mL

0.5785 mL

1.1569 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)

Verweise

[1]. Du Y, et al. HJM-561, a Potent, Selective, and Orally Bioavailable EGFR PROTAC that Overcomes Osimertinib-Resistant EGFR Triple Mutations. Mol Cancer Ther. 2022 Jul 5;21(7):1060-1066. [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	1.1569 mL	5.7846 mL	11.5691 mL	28.9228 mL
	5 mM	0.2314 mL	1.1569 mL	2.3138 mL	5.7846 mL
	10 mM	0.1157 mL	0.5785 mL	1.1569 mL	2.8923 mL
	15 mM	0.0771 mL	0.3856 mL	0.7713 mL	1.9282 mL
	20 mM	0.0578 mL	0.2892 mL	0.5785 mL	1.4461 mL
	25 mM	0.0463 mL	0.2314 mL	0.4628 mL	1.1569 mL
	30 mM	0.0386 mL	0.1928 mL	0.3856 mL	0.9641 mL
	40 mM	0.0289 mL	0.1446 mL	0.2892 mL	0.7231 mL
	50 mM	0.0231 mL	0.1157 mL	0.2314 mL	0.5785 mL
	60 mM	0.0193 mL	0.0964 mL	0.1928 mL	0.4820 mL
	80 mM	0.0145 mL	0.0723 mL	0.1446 mL	0.3615 mL
	100 mM	0.0116 mL	0.0578 mL	0.1157 mL	0.2892 mL

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HJM-561

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

PROTAC Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HJM-561

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

PROTAC Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HJM-561 Related Classifications

HY-156698 Related Classifications