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.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 5 mg | In stock | $ 742 | |
| 10 mg | In stock | $ 1094 | |
| 50 mg | In stock | $ 4384 | |
| 100 mg | In stock | $ 7539 |
| Description | 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. |
| Targets&IC50 | FGFR1: 1.2 nM (IC50); FGFR2: 2.5 nM (IC50); FGFR3: 3.0 nM (IC50); FGFR4: 5.7 nM (IC50); |
| In vitro | 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. |
| 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. |
| CAS No. | 1346242-81-6 |
| Chemical Formula | C25H30N6O2 |
| Molecular Weight | 446.54 |
| Solubility | DMSO: 62.5 mg/mL (139.97 mM, Need ultrasonic) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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