EGFR-TK-IN-4
Based on 1 Customer Validation
EGFR-TK-IN-4 (compound 10k) is a potent and selective EGFR-TK inhibitor. EGFR-TK-IN-4 can induce apoptosis . EGFR-TK-IN-4 has antitumor activity.
For research use only. We do not sell to patients.
- Purity : 99.90%
- CAS No.: 3053485-72-3
- Formula: C23H16F2N6O2S2
- Molecular Weight:510.54
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.82 μM
Compound: 10k
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Anticancer activity against human A549 cells incubated for 72 hrs by MTT assay
Anticancer activity against human A549 cells incubated for 72 hrs by MTT assay
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[PMID: 39094428] |
| BEAS-2B | IC50 |
38.41 μM
Compound: 10k
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Cytotoxicity against human BEAS-2B cells
Cytotoxicity against human BEAS-2B cells
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[PMID: 39094428] |
| HCC827 | IC50 |
0.01 μM
Compound: 10k
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Anticancer activity against human HCC827 cells incubated for 72 hrs by MTT assay
Anticancer activity against human HCC827 cells incubated for 72 hrs by MTT assay
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[PMID: 39094428] |
| NCI-H1975 | IC50 |
0.08 μM
Compound: 10k
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Anticancer activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
Anticancer activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
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[PMID: 39094428] |
Chemical Information
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CAS No. 3053485-72-3
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Appearance Solid
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Molecular Weight 510.54
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Formula C23H16F2N6O2S2
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Color White to off-white
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SMILES
NC1=NC=C(C2=CN=C(SC(C3=CC=CC(NS(C4=CC(F)=CC=C4F)(=O)=O)=C3C)=N5)C5=C2)C=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 (195.87 mM; ultrasonic and warming 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.
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
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Data Sheet (270 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 | 1.9587 mL | 9.7936 mL | 19.5871 mL | 48.9678 mL |
| 5 mM | 0.3917 mL | 1.9587 mL | 3.9174 mL | 9.7936 mL | |
| 10 mM | 0.1959 mL | 0.9794 mL | 1.9587 mL | 4.8968 mL | |
| 15 mM | 0.1306 mL | 0.6529 mL | 1.3058 mL | 3.2645 mL | |
| 20 mM | 0.0979 mL | 0.4897 mL | 0.9794 mL | 2.4484 mL | |
| 25 mM | 0.0783 mL | 0.3917 mL | 0.7835 mL | 1.9587 mL | |
| 30 mM | 0.0653 mL | 0.3265 mL | 0.6529 mL | 1.6323 mL | |
| 40 mM | 0.0490 mL | 0.2448 mL | 0.4897 mL | 1.2242 mL | |
| 50 mM | 0.0392 mL | 0.1959 mL | 0.3917 mL | 0.9794 mL | |
| 60 mM | 0.0326 mL | 0.1632 mL | 0.3265 mL | 0.8161 mL | |
| 80 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6121 mL | |
| 100 mM | 0.0196 mL | 0.0979 mL | 0.1959 mL | 0.4897 mL |
EGFR-TK-IN-4 Related Classifications
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