Art. -Nr.: HY-163726

GLUT1/EGFR-IN-1

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GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research.

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Reinheit: 99.75%
CAS. Nr.: 2393787-80-7
Formel: C₄₄H₃₂N₄O₅
Molecular Weight:696.75

Speicherung:

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

GLUT1/EGFR-IN-1 Chemical Structure

CAS. Nr.: 2393787-80-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

GLUT1

EGFR

Alle GLUT Isoform-spezifische Produkte anzeigen :

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	23.3 μM Compound: 25	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
CNE	IC₅₀	2.1 μM Compound: 25	Antiproliferative activity against human CNE cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human CNE cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
HepG2	IC₅₀	34.9 μM Compound: 25	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
MDA-MB-231	IC₅₀	3.2 μM Compound: 25	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]
SK-OV-3	IC₅₀	12.5 μM Compound: 25	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32739648]

In Vitro

GLUT1/EGFR-IN-1 (compound H) showed outstanding antitumour activity in CNE1 and MDA-MB231 cells, with IC₅₀ values lower than 3 µmol/L, but activity was not obvious in CNE2 cells^[1].
GLUT1/EGFR-IN-1 (0-4 μM, 48 h) inhibits the expression of EGFR and p-EGFR in both CNE1 and MDA-MB231 cells^[1].
GLUT1/EGFR-IN-1 (0-4 μM, 48 h) induces apoptosis in CNE1 and MDA-MB231 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

CNE1 and MDA-MB231 cells
Concentration:

1 μmol/L, 2, 4 μmol/L
Incubation Time:

48 h
Result:

Depressed the expression of EGFR-, p-EGFR- and GLUT1-mediated glycolysis-related proteins.

In Vivo

GLUT1/EGFR-IN-1 (compound H) (4-8 mg/kg, IP, for two weeks) inhibits the growth of the MDA-MB231-transplanted tumour cells in a nude mice model^[1].

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

Animal Model:

BALB/c-neu female mice (Four- to five-week-old, n=5)^[1]
Dosage:

4, 8 mg/kg
Administration:

IP, for two weeks
Result:

Inhibited the growth of the MDA-MB231 transplanted tumour model in nude mice.

Chemical Information

CAS. Nr. 2393787-80-7
Appearance Solid
Molecular Weight 696.75
Formel C₄₄H₃₂N₄O₅
Color Light yellow to yellow
SMILES

O=C(C1=C2C=C(C=C1OCC3=CC=CC=C3)C(NC4=CC=C(C5=C4)N=CN=C5NC6=CC=C(C=C6)C)=O)C7=C(C=CC=C7C2=O)OCC8=CC=CC=C8
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (143.52 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

1.4352 mL

7.1762 mL

14.3524 mL

5 mM

0.2870 mL

1.4352 mL

2.8705 mL

10 mM

0.1435 mL

0.7176 mL

1.4352 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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Wang C, et al. Targeted blocking of EGFR and GLUT1 by compound H reveals a new strategy for treatment of triple-negative breast cancer and nasopharyngeal carcinoma. Eur J Pharm Sci. 2024 Jul 1;198:106789. [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	1.4352 mL	7.1762 mL	14.3524 mL	35.8809 mL
	5 mM	0.2870 mL	1.4352 mL	2.8705 mL	7.1762 mL
	10 mM	0.1435 mL	0.7176 mL	1.4352 mL	3.5881 mL
	15 mM	0.0957 mL	0.4784 mL	0.9568 mL	2.3921 mL
	20 mM	0.0718 mL	0.3588 mL	0.7176 mL	1.7940 mL
	25 mM	0.0574 mL	0.2870 mL	0.5741 mL	1.4352 mL
	30 mM	0.0478 mL	0.2392 mL	0.4784 mL	1.1960 mL
	40 mM	0.0359 mL	0.1794 mL	0.3588 mL	0.8970 mL
	50 mM	0.0287 mL	0.1435 mL	0.2870 mL	0.7176 mL
	60 mM	0.0239 mL	0.1196 mL	0.2392 mL	0.5980 mL
	80 mM	0.0179 mL	0.0897 mL	0.1794 mL	0.4485 mL
	100 mM	0.0144 mL	0.0718 mL	0.1435 mL	0.3588 mL

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GLUT1/EGFR-IN-1

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Membrane Transporter/Ion Channel Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Glycolysis Compound Library

Glutamine Metabolism Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alle GLUT 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

GLUT1/EGFR-IN-1 Related Classifications

HY-163726 Related Classifications