Erdafitinib is a fibroblast growth factor receptor inhibitor. Erdafitinib (JNJ-42756493) inhibits the tyrosine kinase activities of FGFR1-4 in time-resolved fluorescence assays with IC50 values of 1.2, 2.5, 3.0 and 5.7nM, respectively. The closely related VEGFR2 kinase is less potently inhibited (30-fold less potent compared to FGFR1) by erdafitinib, with an IC50 value of 36.8nM. Erdafitinib binds FGFR1, 3, 4, and 2 with Kd values of 0.24, 1.1, 1.4 and 2.2nM, respectively. The Kd value for VEGFR2 is higher at 6.6nM. Erdafitinib inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively[1]. In xenografts from human tumor cell lines or patient-derived tumor tissue with activating FGFR alterations, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors[1]. Synonyms: N1-(3,5-Dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine, JNJ 42756493 CAS No: 1346242-81-6 Molecular Formula: C25H30N6O2 Molecular Weight: 446.54 Purity (LCMS): 99% Appearance: Light yellow to yellow solid Melting Point: 136-140C H NMR Spectrum: Conforms with structure LCMS: Conforms with structure Solubility: DMSO (Slightly), Methanol (Slightly) Storage and Stability: Store at -20C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Molekulargewicht:
446.54
Reinheit:
99%
Formulierung:
Yellow solid
CAS Nummer:
[1346242-81-6]
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