All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Biological Description

Description: Erdafitinib is a quinoxaline derivative compound, acts on FGFR1/2/3/4.

Targets&IC50: FGFR4:5.7 nM, FGFR3:3.0nM, FGFR1:1.2 nM, FGFR2:2.5nM

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.

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.

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)

Chemical Properties

Molecular Weight: 446.555

Formula: C25H30N6O2

CAS No.: 1346242-81-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 15 mg/mL(33.6 mM)

H2O: <1 mg/mL

DMSO: 82 mg/mL (183.6 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Catalog #: T3726

Please email us at cs@medikonia.com for any enquiry. To place an order, please include the catalog number(s) of the product(s) in the email.

References and Literature

1. Timothy Perera, et al. Cancer Res. 2014, 74(19 Suppl):Abstract nr 1738.

2. Verstraete M, et al. BMC Cancer. 2015, 15:946.