Mefatinib
Based on 1 Customer Validation
Mefatinib (Mifanertinib dimaleate) is an orally active EGFR and HER2 kinase inhibitor with IC50 values of 0.4 nM and 11.7 nM, respectively. Mefatinib inhibits tumor growth in mouse models of lung cancer xenografts that overexpress EGFR/HER2, carry EGFR mutations, or carry Erlotinib (HY-50896)-resistant EGFR double mutations. Mefatinib can be used for the research of advanced EGFR-mutant non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity : 99.44%
- CAS No.: 1989592-50-8
- Formula: C29H27ClF3N5O10
- Molecular Weight:698.00
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All EGFR Isoforms
More
Biological Activity
Description
IC50 & Target
|
EGFR 0.4 nM (IC50) |
HER2 11.7 nM (IC50) |
In Vivo
Mefatinib (0.2 mg/kg) achieves 99.6% tumor growth inhibition in a nude mouse xenograft model of human lung adenocarcinoma HCC827[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1989592-50-8
-
Appearance Solid
-
Molecular Weight 698.00
-
Formula C29H27ClF3N5O10
-
Color Off-white to light yellow
-
SMILES
OC(/C=C\C(O)=O)=O.O=C(NC1=CC2=C(NC3=CC=C(C(Cl)=C3)F)N=CN=C2C=C1OC(F)F)/C=C/CN(C)C.OC(/C=C\C(O)=O)=O
-
Synonyms
Mifanertinib dimaleate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
H2O : 100 mg/mL (143.27 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
-
Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
-
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.
-
Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.4327 mL | 7.1633 mL | 14.3266 mL | 35.8166 mL |
| 5 mM | 0.2865 mL | 1.4327 mL | 2.8653 mL | 7.1633 mL | |
| 10 mM | 0.1433 mL | 0.7163 mL | 1.4327 mL | 3.5817 mL | |
| 15 mM | 0.0955 mL | 0.4776 mL | 0.9551 mL | 2.3878 mL | |
| 20 mM | 0.0716 mL | 0.3582 mL | 0.7163 mL | 1.7908 mL | |
| 25 mM | 0.0573 mL | 0.2865 mL | 0.5731 mL | 1.4327 mL | |
| 30 mM | 0.0478 mL | 0.2388 mL | 0.4776 mL | 1.1939 mL | |
| 40 mM | 0.0358 mL | 0.1791 mL | 0.3582 mL | 0.8954 mL | |
| 50 mM | 0.0287 mL | 0.1433 mL | 0.2865 mL | 0.7163 mL | |
| 60 mM | 0.0239 mL | 0.1194 mL | 0.2388 mL | 0.5969 mL | |
| 80 mM | 0.0179 mL | 0.0895 mL | 0.1791 mL | 0.4477 mL | |
| 100 mM | 0.0143 mL | 0.0716 mL | 0.1433 mL | 0.3582 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.