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Erdafitinib — Datasheet

CAT. NO. DC11387

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ParameterValue
Chemical NameErdafitinib
CAS No.1346242-81-6
SynonymsErdafitinib;N1-(3,5-Dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine;Erdafitinib(JNJ-42756493);890E37NHMV;N'-(3,5-dimethoxyphenyl)-N'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-N-propan-2-ylethane-1,2-diamine;Erdafitinib [USAN:INN];Erdafitinib (USAN/INN);GTPL9039;BCP20346;s8401;compound 4 [WO2011135376];SB16854;DB12147;JNJ42756493;N-(3,5-dimethoxyphenyl
FormulaC25H30N6O2
M.Wt446.5447
SMILESO(C([H])([H])[H])C1C([H])=C(C([H])=C(C=1[H])N(C1C([H])=C([H])C2C(C=1[H])=NC(C1C([H])=NN(C([H])([H])[H])C=1[H])=C([H])N=2)C([H])([H])C([H])([H])N([H])C([H])(C([H])([H])[H])C([H])([H])[H])OC([H])([H])[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

In Vitro

Erdafitinib inhibits the tyrosine kinase activities of FGFR1-4 in time-resolved fluorescence assays with IC50 values of 1.2, 2.5, 3.0 and 5.7 nM, respectively. The closely related VEGFR2 kinase is less potently inhibited (30-fold less potent compared to FGFR1) by erdafitinib, with an IC50 value of 36.8 nM. JNJ-42756493 binds FGFR1, 3, 4, and 2 with Kd values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The Kd value for VEGFR2 is higher at 6.6 nM. JNJ-42756493 inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively[1].

In Vivo

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].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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