EAI045
Based on 3 publication(s) in Google Scholar
EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.
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- Pureza: 99.06%
- No. CAS: 1942114-09-1
- Fòrmula: C19H14FN3O3S
- Peso molecular:383.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) EAI045
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Actividad biológica
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EGFR 1.9 μM (IC50) |
EGFRL858R 0.019 μM (IC50) |
EGFRT790M 0.19 μM (IC50) |
EGFRL858R/T790M 0.002 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
1.9 μM
Compound: EAI045
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Antiproliferative activity against human A-431 cells expressing wild type EGFR assessed as inhibition of cell growth
Antiproliferative activity against human A-431 cells expressing wild type EGFR assessed as inhibition of cell growth
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[PMID: 35728507] |
| BaF3 | IC50 |
~ 10 nM
Compound: 1; EAI045
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Inhibition of cell proliferation in mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by MTS assay
Inhibition of cell proliferation in mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by MTS assay
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[PMID: 38908104] |
| BaF3 | IC50 |
>10 μM
Compound: 1; EAI045
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Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay
Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay
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[PMID: 31223440] |
| BaF3 | IC50 |
>10 μM
Compound: 1; EAI045
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth
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[PMID: 35378251] |
| BaF3 | IC50 |
>10000 nM
Compound: 20; EAI045
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Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
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[PMID: 36417820] |
| BaF3 | IC50 |
>10000 nM
Compound: 20; EAI045
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Cytotoxicity against mouse BaF3 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 36417820] |
| BaF3 | IC50 |
0.221 μM
Compound: 1; EAI045
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth in presence of cetuximab
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth in presence of cetuximab
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[PMID: 35378251] |
| NCI-H1975 | IC50 |
2 nM
Compound: EAI045
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Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth
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[PMID: 35728507] |
| Sf9 | IC50 |
3 nM
Compound: EAI045
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Inhibition of human EGFR L858R/T790M mutant (696 to 1022 residues) expressed in Sf9 insect cells by HTRF assay
Inhibition of human EGFR L858R/T790M mutant (696 to 1022 residues) expressed in Sf9 insect cells by HTRF assay
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[PMID: 31274316] |
| Sf9 | IC50 |
73.1 nM
Compound: 2a; EAI045
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Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA
Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA
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[PMID: 31298540] |
EAI045 potently inhibits EGFR Y1173 phosphorylation in H1975 cells (EC50=2 nM), but not in HaCaT cells. EAI045 is an inhibitor of the L858R/T790M mutant with 1000-fold selectivity versus wild type EGFR at 1 mM ATP. Profiling of EAI045 against a panel of 250 protein kinases reveals exquisite selectivity; no other kinases are inhibited by more than 20% at 1 μM EAI045[1]. EAI045 has high potency and selectivity for L858R/T790M mutation. In L858R/T790M-mutant NSCLC cell line H1975 cells, EAI045 decreases but does not completely abolish the EGFR autophosphorylation. In stably transfected NIH-3T3 cells harboring the L858R/T790M EGFR mutant, EAI045 shows the same activity. In L858R-mutant H3255 cells, EAI045 exhibits moderate activity. In the HaCaT cells, a keratinocyte cell line with wild-type EGFR, EAI045 does not show any activity of inhibiting EGFR phosphorylation. It confirms the selectivity of EAI045 for mutant EGFR[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1942114-09-1
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Appearance Solid
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Peso molecular 383.40
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Fòrmula C19H14FN3O3S
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Color White to khaki
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SMILES
O=C(C(C1=C(O)C=CC(F)=C1)N2C(C(C=CC=C3)=C3C2)=O)NC4=NC=CS4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cancer Lett
2025 Jul 28:623:217715. PMID: 40220852 -
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J Chromatogr Sci
A Validated LC Method for the Enantiomeric Separation of EAI045 on Chiral Stationary Phase. [Abstract]2020 Jun 5;58(6):562-568. PMID: 32303742
Solvente y solubilidad
DMSO : 100 mg/mL (260.82 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.52 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.52 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
For the experiment studying the effect of EGF pre-treatment on EAI045 target modulation, H1975 cells are harvested and plated in 0.5% FBS/RPMI Pen/Strep. On the following day, cells are pre-treated with 0.5% FBS/RPMI media with or without 10 ng EGF/mL for 5 minutes. Compound is added and assay is carried out[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Cetuximab is administrated at 1 mg/mouse every other day by intraperitoneal injection. The TL, TD and TLCS mice are monitored by MRI to quantify lung tumor burden before being assigned to various study treatment cohorts, which are non-blinded and not formally randomized. All treated mice had an equal initial tumor burden. MRI evaluation is repeated every 2 weeks during treatment. The animals are imaged with a rapid acquisition with relaxation enhancement sequence in the coronal and axial planes with a 1-mm slice thickness gating with respiratory rates. The tumor burden volumes are quantified[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jia Y, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32. [Content Brief]
[2]. Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL | 65.2061 mL |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL | 13.0412 mL | |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL | 6.5206 mL | |
| 15 mM | 0.1739 mL | 0.8694 mL | 1.7388 mL | 4.3471 mL | |
| 20 mM | 0.1304 mL | 0.6521 mL | 1.3041 mL | 3.2603 mL | |
| 25 mM | 0.1043 mL | 0.5216 mL | 1.0433 mL | 2.6082 mL | |
| 30 mM | 0.0869 mL | 0.4347 mL | 0.8694 mL | 2.1735 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6521 mL | 1.6302 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.3041 mL | |
| 60 mM | 0.0435 mL | 0.2174 mL | 0.4347 mL | 1.0868 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8151 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6521 mL |
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