Erdafitinib 是一种喹喔啉衍生物，是一种具有口服活性的FGFR家族抑制剂，抑制FGFR1/2/3/4活性的IC50分别为1.2、 2.5、3.0和5.7 nM。

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

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[2].

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[2]. 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[1].

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)

1346242-81-6

C25H30N6O2

446.555

厄达替尼;JNJ-42756493

DMSO:82 mg/mL (183.6 mM)
Ethanol:15 mg/mL(33.6 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years