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Submit ReviewJBJ-03-142-02
Description: Highly potent EGFR and ErbB2 inhibitor; inhibts wild type and mutated receptors
Chemical Name: (4-Fluorophenyl)methyl N-[2-[(1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-N-[3-[(1-oxo-2-propen-1-yl)amino]phenyl]carbamate
Purity: ≥98% (HPLC)
Biological Activity for JBJ-03-142-02
JBJ-03-142-02 is a highly potent epidermal growth factor receptor (EGFR) and ErbB2 (human epidermal growth factor receptor; HER2) inhibitor. Inhibits wild type and tumorgenic mutated receptors (exon 20 insertion; Ex20Ins). Antiproliferative in vitro (IC50 values are 7.6, 30 - 95, 3.8 and 19 - 31 nM for Ba/F3 cells expressing wild type EGFR, EGFR with Ex20Ins mutation, wild type HER2 and HER2 with Ex20Ins mutation, respectively). Also inhibits other common EGFR mutants. Antiproliferative in patient-derived lung cancer cell lines.
Licensing Information
Sold under license from Dana-Farber Cancer Institute
Technical Data for JBJ-03-142-02
| M. Wt | 487.5 |
| Formula | C25H22FN7O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2068806-31-3 |
| PubChem ID | 126496758 |
| InChI Key | IFRXGTCPIGRGHP-UHFFFAOYSA-N |
| Smiles | CN1C=C(NC2=NC=CC(=N2)N(C(=O)OCC2=CC=C(F)C=C2)C2=CC(NC(=O)C=C)=CC=C2)C=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JBJ-03-142-02
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.37 | 50 |
Preparing Stock Solutions for JBJ-03-142-02
The following data is based on the product molecular weight 487.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.1 mL | 20.51 mL | 41.03 mL |
| 2.5 mM | 0.82 mL | 4.1 mL | 8.21 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.1 mL |
| 25 mM | 0.08 mL | 0.41 mL | 0.82 mL |
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Product Datasheets for JBJ-03-142-02
References for JBJ-03-142-02
References are publications that support the biological activity of the product.
Jang et al (2018) Discovery of a highly potent and broadly effective epidermal growth factor receptor and HER2 exon 20 insertion mutant inhibitor. Angew.Chem.Int.Ed.Engl. 57 11629 PMID: 29978938
If you know of a relevant reference for JBJ-03-142-02, please let us know.
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Keywords: JBJ-03-142-02, JBJ-03-142-02 supplier, JBJ0314202, mutated, EGFR, GER2, ErbB2, inhibitors, inhibits, highly, potent, epidermal, growth, factor, receptor, 6962, Tocris Bioscience
Citations for JBJ-03-142-02
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