Erdafitinib

• CAT Number: I001324
• CAS Number: 1346242-81-6
• Molecular Formula: C25H30N6O2
• Molecular Weight: 446.5
• Purity: ≥95%
• Target: FGFR
• Solubility: DMSO: ≥ 33 mg/mL
• Storage: -20°C
• IC50: 9/8.5/8.5/8.25 (pIC50, for FGFR1/2/3/4)
• 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: COC1=CC(OC)=CC(N(CCNC(C)C)C2=CC=C(N=CC(C3=CN(C)N=C3)=N4)C4=C2)=C1

Erdafitinib,(CAT: I001324) is a potent and selective inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinases. By targeting FGFRs, erdafitinib interferes with aberrant signaling pathways involved in cell growth, survival, and angiogenesis. This pharmacologic action makes erdafitinib particularly effective against cancers harboring specific FGFR genetic alterations, such as FGFR2 fusions or mutations. Erdafitinib has demonstrated clinical efficacy in the treatment of metastatic urothelial carcinoma, providing a targeted therapeutic option for patients with these genetic alterations.

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