Erdafitinib chemical structure
Chemical structureResearch use only
CAT. NO. DC11387Featured

Erdafitinib

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Product overview

Description & Application

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.

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.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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