ERDAFITINIB

💡1.Basic Information

Erdafitinib, the English name for it is Erdafitinib, and it is also known as JNJ-42756493.Erdafitinib, the English name for it is Erdafitinib, and it is also known as JNJ-42756493. Its commercial name is Balversa®. Its commercial name is Balversa®. The CAS number is 1346242-81-6. The CAS number is 1346242-81-6. Its molecular formula is C₂₅H₃₀N₆O₂ and its molecular weight is 446.54 g/mol. Its molecular formula is C₂₅H₃₀N₆O₂ and its molecular weight is 446.54 g/mol. The product appears as a white to off-white solid powder. The product appears as a white to off-white solid powder. The common purity specification is over 98%.
The common purity specification is over 98%.
The chemical name of eradatinib is N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinol-6-yl)ethane-1,2-diamine.The chemical name of eradatinib is N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinol-6-yl)ethane-1,2-diamine.

👨‍🔬2.Mechanism of action and targets

Erdafitinib is an oral, selective, pan-FGFR (fibroblast growth factor receptor) tyrosine kinase inhibitor, belonging to a class of small molecule targeted anti-tumor drugs. The inhibitory activity of this drug on each member of the FGFR family is as follows: the IC₅₀ for FGFR1 is 1.
2 nM, for FGFR2 it is 2.5 nM, for FGFR3 it is 3.The inhibitory activity of this drug on each member of the FGFR family is as follows: the IC₅₀ for FGFR1 is 1.2 nM, for FGFR2 it is 2.50 nM, and for FGFR4 it is 5.7 nM. nM, for FGFR3 it is 3.0 nM, and for FGFR4 it is 5.7 nM. Erdatainib has high selectivity for the FGFR family and has a relatively weak inhibitory activity on VEGFR2 (IC₅₀ is approximately 36. Erdatini has high selectivity for the FGFR family and has a relatively weak inhibitory activity on VEGFR2 (IC₅₀ is approximately 36.8 nM), which is about 30 times weaker than its inhibitory activity on FGFR1.8 nM), which is about 30 times weaker than its inhibitory activity on FGFR1.

Mechanism of action: Erdafitinib achieves its effect by reversibly binding to and inhibiting the enzymatic activity of FGFR1-4, blocking the signaling pathways related to FGFR, thereby inhibiting the proliferation of tumor cells with FGFR gene mutations (including point mutations, amplification, and fusion), and inducing cell apoptosis.Mechanism of action: Erdafitinib achieves its effect by reversibly binding to and inhibiting the enzymatic activity of FGFR1-4, blocking the signaling pathways related to FGFR, thereby inhibiting the proliferation of tumor cells with FGFR gene mutations (including point mutations, amplification, and fusion), and inducing cell apoptosis.

🔍3.Storage conditions

The storage requirements for eradatinib vary depending on its form:
Powder form: It can be stably stored for 3 years at -20°C and for 2 years at 4°C. It should be stored in a dark place, protected from moisture, and kept in a sealed and dry environment.
Solution form (e.g. DMSO dissolution): Stable for 6 months at -80°C and 1 month at -20°C. It is recommended to store in aliquots to avoid repeated freezing and thawing.

📊4.Scientific research application

In vitro study: Erdatainib can effectively inhibit the proliferation of FGFR-dependent tumor cells in vitro. At a concentration of 0.5 nM, it can significantly reduce cell growth and survival rate in colorectal cancer cells NCI-H716. In various tumor cell lines, Erdatainib can effectively inhibit the autophosphorylation of FGFR1, FGFR2, FGFR3, and FGFR4, with the IC₅₀ value ranging from 30 to 100 nM.
In vivo study: In a mouse tumor transplantation model, oral administration of eradatin (40 mg/kg, three times a week) significantly inhibited tumor growth. In the NCI-H716 colorectal cancer model, the tumor volume increased by only 24.1% after one week of treatment, while the control group increased by 88.2%. Eradatin is widely distributed in lung, liver and kidney tissues and exhibits dose-dependent anti-tumor activity.

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