2. Membrane Transporter/Ion Channel Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. GLUT EGFR Apoptosis
  4. GLUT1/EGFR-IN-1

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.

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

GLUT1/EGFR-IN-1 Chemical Structure

GLUT1/EGFR-IN-1 Chemical Structure

CAS No. : 2393787-80-7

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Based on 1 publication(s) in Google Scholar

GLUT1/EGFR-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target

GLUT1

 

EGFR

 

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.

GLUT1/EGFR-IN-1 Related Antibodies

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.
Molecular Weight

696.75

Formula

C44H32N4O5
CAS No.
Appearance

Solid

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
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 (143.52 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 1.4352 mL 7.1762 mL 14.3524 mL
5 mM 0.2870 mL 1.4352 mL 2.8705 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 1.4352 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 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.

Keywords:

GLUT1/EGFR-IN-12393787-80-7GLUTEGFRApoptosisGlucose transporter Epidermal growth factor receptorErbB-1HER1anti-tumor activityCNE1MDA-MB231nasopharyngeal carcinomatriple-negative breast cancerInhibitorinhibitorinhibit

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