EGFR-IN-7
Based on 1 Customer Validation
EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.59%
- CAS No.: 2267329-76-8
- Formule: C32H41BrN9O2P
- Masse moléculaire:694.60
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
EGFR (WT) 7.92 nM (IC50) |
EGFR (C797S/T790M/L858R) 0.218 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
17 nM
Compound: TQB3804
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Antiproliferative activity against mouse BaF3 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
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[PMID: 35254067] |
| BaF3 | IC50 |
21 nM
Compound: TQB3804
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Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
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[PMID: 35254067] |
| NCI-H1975 | IC50 |
910 nM
Compound: TQB3804
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Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
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[PMID: 35254067] |
| PC-9 | IC50 |
45 nM
Compound: TQB3804
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Antiproliferative activity against human PC-9 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-9 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth growth incubated for 72 hrs by MTT assay
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[PMID: 35254067] |
In Vitro
EGFR-IN-7 (compound 34) (10 mM) has a strong inhibitory effect on the enzymatic activity of EGFR (WT), EGFR (Δ19del/T790M/C797S) and EGFR (C797S/T790M/L858R) with IC50 values of 7.92 nM, 0.218 nM and 0.16 nM, respectively[1].
EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC50 value of 154 nM[1].
EGFR-IN-7 (10 μM-0.508 nM) has a good inhibitory effect on cells of the Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant with an IC50 value of 22 nM[1].
EGFR-IN-7 (10 μM or 100 μM) has inhibition of phosphorylation activity of pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells with an IC50 value of 19 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A431 cells; Ba/F 3 (EGFRΔ19del/T790M/C797S) suspension cells
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Concentration:1 mM; 10 μM-0.508 nM
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Incubation Time:3 days
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Result:Inhibited proliferation in cells.
In Vivo
EGFR-IN-7 (25 and 50 mg/kg; p.o.; daily, for 3 weeks) has a significant inhibitory effect on tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)[1]
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Dosage:5, 15, 45 mg/kg
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Administration:Oral administration, daily, for 13 days
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Result:Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice.
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Animal Model:Subcutaneous xenograft PC-9 (Δ19del) model[1]
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Dosage:0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg
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Administration:Oral administration, once a day, 3 weeks
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Result:Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy.
Chemical Information
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CAS No. 2267329-76-8
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Appearance Solid
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Masse moléculaire 694.60
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Formule C32H41BrN9O2P
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Color Light yellow to yellow
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SMILES
CN1CCN(C2CCN(C3=C(C)C=C(NC4=NC=C(Br)C(NC5=CC=C6N=CC=NC6=C5P(C)(C)=O)=N4)C(OC)=C3)CC2)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 5 mg/mL (7.20 mM; ultrasonic and warming and adjust pH to 5 with 0.1 M HCl and heat to 60°C; 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)
In Vivo:
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: ≥ 1.25 mg/mL (1.80 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (1.80 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
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.
Pureté et documentation
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Fiche technique (273 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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Instruction de manipulation (2659 KB)
Références
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 | 1.4397 mL | 7.1984 mL | 14.3968 mL | 35.9919 mL |
| 5 mM | 0.2879 mL | 1.4397 mL | 2.8794 mL | 7.1984 mL |
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