Erdafitinib

• CAT Number: I001324
• CAS Number: 1346242-81-6
• Molecular Formula: C25H30N6O2
• Molecular Weight: 446.50
• Purity: 98%
• Synonyms: Erdafitinib
• Target: Apoptosis
• Target Protein: P11362,P21802,P22607
• Solubility: DMSO: ≥ 33 mg/mL
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: FGFR1：1.2 nM (IC50)
• IUPAC Name: N'-(3,5-dimethoxyphenyl)-N'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-N-propan-2-ylethane-1,2-diamine
• InChI: InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
• InChIKey: OLAHOMJCDNXHFI-UHFFFAOYSA-N
• SMILES: CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC

Erdafitinib（Cat No.:I001324）is an oral tyrosine kinase inhibitor that targets fibroblast growth factor receptors (FGFR1-4), playing a critical role in cancer cell proliferation and survival. It is primarily used for treating locally advanced or metastatic urothelial carcinoma with susceptible FGFR genetic alterations. By inhibiting FGFR signaling, erdafitinib blocks tumor growth and angiogenesis, offering a therapeutic option for patients with limited treatment alternatives. Its targeted mechanism of action provides a personalized approach to cancer therapy, particularly for those with FGFR-driven malignancies, improving treatment outcomes in advanced cancer stages.

Reference

1:Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib. Karkera JD, Martinez Cardona G, Bell K, Gaffney D, Portale JC, Santiago-Walker A, Moy C, King P, Sharp M, Bahleda R, Luo FR, Alvarez JD, Lorenzi MV, Platero SJ.Mol Cancer Ther. 2017 Apr 17. pii: molcanther.0518.2016. doi: 10.1158/1535-7163.MCT-16-0518. [Epub ahead of print] PMID: 28416604
2:Discovery and pharmacological characterization of JNJ-42756493 (erdafitinib), a functionally selective small molecule FGFR family inhibitor. Perera TP, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Gilissen R, Murray CW, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV.Mol Cancer Ther. 2017 Mar 24. pii: molcanther.0589.2016. doi: 10.1158/1535-7163.MCT-16-0589. [Epub ahead of print] PMID: 28341788