GLUT1/EGFR-IN-1
Based on 1 Customer Validation
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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- Purity : 99.75%
- CAS No.: 2393787-80-7
- 화학식: C44H32N4O5
- 분자량:696.75
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All EGFR Isoforms
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Biological Activity
제품 설명
IC50 & Target
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GLUT1 |
EGFR |
Cellular Effect
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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. Further protocols information, click here.
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Cell Line:CNE1 and MDA-MB231 cells
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Concentration:1 μmol/L, 2, 4 μmol/L
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Incubation Time:48 h
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Result:Depressed the expression of EGFR-, p-EGFR- and GLUT1-mediated glycolysis-related proteins.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-neu female mice (Four- to five-week-old, n=5)[1]
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Dosage:4, 8 mg/kg
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Administration:IP, for two weeks
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Result:Inhibited the growth of the MDA-MB231 transplanted tumour model in nude mice.
Chemical Information
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CAS No. 2393787-80-7
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Appearance Solid
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분자량 696.75
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화학식 C44H32N4O5
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Color Light yellow to yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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Mitochondrial membrane-potential fluorescent assay
Mitochondrial membrane potential fluorescent assays estimate ΔΨm in living cells using lipophilic cationic dyes such as TMRM, TMRE, rhodamine 123, and JC-1, which accumulate in mitochondria according to membrane polarization; loss of signal after FCCP or CCCP treatment is interpreted as mitochondrial depolarization. TMRM/TMRE and rhodamine 123 are commonly used for semi-quantitative live-cell microscopy or flow cytometry, while JC-1 can report a shift from red aggregate fluorescence to green monomer fluorescence during depolarization; interpretation requires controls because dye concentration, quenching mode, cell type, dye efflux, and mitochondrial mass can affect fluorescence independently of ΔΨm.
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Human pluripotent stem cell neural induction and neuron differentiation
Human pluripotent stem cell neural induction can be achieved by blocking BMP and TGFβ/Activin/Nodal SMAD signaling, which suppresses non-neural differentiation and promotes early neuroectodermal identity; the expected readout is loss of pluripotency markers such as OCT4 and induction of neural markers such as PAX6, followed by neural progenitor and neuron marker acquisition during differentiation. This protocol uses dual-SMAD neural induction as the core induction method, followed by cortical neuron differentiation as a representative neuron differentiation model; published cortical protocols describe generation of cortical progenitors, temporally ordered cortical projection neurons, action-potential firing, synaptogenesis, and neural network formation over an approximately 80-day process.
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Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
순도&문서
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Data Sheet (275 KB)
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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)
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Handling Instructions (2659 KB)
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 |