JNJ-42756493 MedChemExpress (MCE)

Product Name	ERDAFITINIB
Synonyms	Erdafitinib ERDAFITINIB JNJ-42756493 Suftalan Zine Erdafitinib(JNJ-42756493) N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine N1-(3,5-Dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine
CAS	1346242-81-6
EINECS
Chemical Formula	C25H30N6O2
Molecular Weight	446.5447
inchi
Package	10 mM * 1 mL;10 mM * 1 mL;1 mg;1 mg;5 mg;5 mg;10 mg;10 mg;25 mg;25 mg
Price	Email to quote
Descriptions	Erdafitinib Erdafitinib MedChemExpress (MCE) HY-18708 1346242-81-6 JNJ-42756493 99.66% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Erdafitinib Erdafitinib MedChemExpress (MCE) HY-18708 1346242-81-6 JNJ-42756493 99.66% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. 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. 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 5.7 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. Erdafitinib 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. 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]. Mice: Mice bearing SNU-16 human gastric carcinoma (FGFR2 amplified) xenograft tumors are dosed orally with 0, 3, 10 or 30 mg/kg Erdafitinib. Tumor tissue and mouse plasma (3 mice per time point) are harvested at 0.5, 1, 3, 7, 16 and 24h post-dosing[1]. Erdafitinib is dissolved in DMSO. KATO III, RT-112, A-204, RT-4, DMS-114, A-427 and MDA-MB-453 cells are treated with erdafitinib (from 10 μM to 0.01 nM in 2% DMSO, final concentration). Following 4-day incubation, cell viability is determined using MTT reagent. The optical density is determined at 540 nm[1]. FGFR1 1.2 nM (IC50) FGFR2 2.5 nM (IC50) FGFR3 3.0 nM (IC50) FGFR4 5.7 nM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Perera TP, et al. Discovery and pharmacological characterization of JNJ-42756493 (erdafitinib), a functionally selective small molecule FGFR family inhibitor. Mol Cancer Ther. 2017 Mar 24. pii: molcanther.0589.2016. [Content Brief]
Last Update	2025-04-01 14:45:47

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