JBJ-03-142-02

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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)
Datasheet
Citations
Reviews
Literature (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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


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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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Literature in this Area

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Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.