Erdafitinib

SKU: orb1303841

Description

Erdafitinib (JNJ-42756493) is a potent, pan-FGFR inhibitor targeting FGFR1-4 with low nanomolar IC50 values. It demonstrates pro-apoptotic and antitumor effects, supporting its research use in oncology for both in vitro cellular studies and in vivo xenograft models of FGFR-altered cancers.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1346242-81-6
• MW: 446.54
• Purity: 99.36%
• Formula: C₂₅H₃₀N₆O₂
• SMILES: COc1cc(OC)cc(c1)N(CCNC(C)C)c1ccc2ncc(nc2c1)-c1cnn(C)c1
• Target: Apoptosis,FGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:8.2 mg/mL (18.36 mM);Ethanol:15 mg/mL (33.59 mM);DMSO:32 mg/mL (71.66 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  FGFR2:2.5nM|FGFR4:5.7 nM|FGFR3:3.0nM|FGFR1:1.2 nM
• In Vivo:
  In vivo, growth of NCI-H716 tumors is delayed by 5 days by drug treatment alone, although when drug delivery is stopped the relative tumor volume increased compared to control. JNJ-42756493 shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. JNJ-42756493 is well tolerated at efficacious doses and results in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components.
• In Vitro:
  JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival.
• Cell Research:
  The effect of varying drug concentrations on cell growth and survival is evaluated at 72 h using sulforhodamine B (SRB) assay for the adherent cells (HCT116, HCA7, Caco2) and trypan blue dye exclusion for the suspension cells, NCI-H716. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, Inhibitor, FGFR4, FGFR, FGFR1, FGFR2, FGFR3, Fibroblast growth factor receptor, Erdafitinib, JNJ 42756493, JNJ42756493, JNJ-42756493, inhibit

Compound Identifiers

PubChem CID

67462786